Alvocidib

Identification

Name

Alvocidib

Accession Number

DB03496

Description

Alvocidib is a synthetic flavonoid based on an extract from an Indian plant for the potential treatment of cancer. It works by inhibiting cyclin-dependent kinases, arresting cell division and causing apoptosis in non-small lung cancer cells.

Type

Small Molecule

Groups

Experimental, Investigational

Structure

Similar Structures

Weight: Average: 401.84
Monoisotopic: 401.103000462
Chemical Formula: C₂₁H₂₀ClNO₅

Synonyms

alvocidib
Alvocidib freebase
Flavopiridol

External IDs

L86-8275

Pharmacology

Indication

Investigated for use/treatment in esophageal cancer, leukemia (lymphoid), lung cancer, liver cancer, and lymphoma (unspecified).

Contraindications & Blackbox Warnings

Learn about our commercial Contraindications & Blackbox Warnings data.

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Pharmacodynamics

Not Available

Mechanism of action

Inhibits cyclin-dependent kinases, arresting cell division and causing apoptosis in non-small lung cancer cells.

Target	Actions	Organism
UCyclin-dependent kinase 2	inhibitor	Humans
UCyclin-dependent kinase 5	Not Available	Humans
UCyclin-dependent kinase 9	Not Available	Humans
UCyclin-dependent kinase 1	Not Available	Humans
UCyclin-dependent kinase 6	Not Available	Humans
UEpidermal growth factor receptor	Not Available	Humans
UCyclin-dependent kinase 4	Not Available	Humans
UCyclin-dependent kinase 8	Not Available	Humans
UCyclin-dependent kinase 7	Not Available	Humans
UGlycogen phosphorylase, muscle form	Not Available	Humans
UGlycogen phosphorylase, brain form	Not Available	Humans
UGlycogen phosphorylase, liver form	Not Available	Humans

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects

Learn about our commercial Adverse Effects data.

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Toxicity

Not Available

Affected organisms

Not Available

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
Unlock Additional Data
Abemaciclib	Abemaciclib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Adenine	The metabolism of Alvocidib can be decreased when combined with Adenine.
Afatinib	Afatinib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Alectinib	Alectinib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Amitriptyline	The metabolism of Alvocidib can be decreased when combined with Amitriptyline.
Apalutamide	Apalutamide may increase the excretion rate of Alvocidib which could result in a lower serum level and potentially a reduction in efficacy.
Atazanavir	The metabolism of Alvocidib can be decreased when combined with Atazanavir.
Avatrombopag	Avatrombopag may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Baricitinib	Baricitinib may decrease the excretion rate of Alvocidib which could result in a higher serum level.
Beclomethasone dipropionate	Beclomethasone dipropionate may decrease the excretion rate of Alvocidib which could result in a higher serum level.

Additional Data Available

Extended Description

Available for Purchase

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

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A severity rating for each drug interaction, from minor to major.

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Evidence Level

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A rating for the strength of the evidence supporting each drug interaction.

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Action

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An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Not Available

Products

Product Ingredients

Ingredient	UNII	CAS	InChI Key
Alvocidib hydrochloride	D48MS3A6N9	131740-09-5	LGMSNQNWOCSPIK-LWHGMNCYSA-N

Chemical Identifiers

UNII: 45AD6X575G
CAS number: 146426-40-6
InChI Key: BIIVYFLTOXDAOV-YVEFUNNKSA-N
InChI: InChI=1S/C21H20ClNO5/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3/t12-,17+/m0/s1
IUPAC Name: 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]-4H-chromen-4-one
SMILES: CN1CC[C@@H]([C@H](O)C1)C1=C(O)C=C(O)C2=C1OC(=CC2=O)C1=CC=CC=C1Cl

References

Synthesis Reference

Kyoung Soon Kim, "Process for the preparation of chiral ketone intermediates useful for the preparation of flavopiridol and analogs." U.S. Patent US5908934, issued March, 1998.

US5908934

General References

Not Available

External Links

PubChem Compound: 5287969
PubChem Substance: 46507266
ChemSpider: 4450222
BindingDB: 5655
ChEBI: 47344
ChEMBL: CHEMBL428690
ZINC: ZINC000021288966
Therapeutic Targets Database: DCL000422
PharmGKB: PA452627
PDBe Ligand: CPB
Wikipedia: Alvocidib

PDB Entries

1c8k / 1e1y / 3blr / 3ebp / 4o71

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
2	Active Not Recruiting	Treatment	Acute Myeloid Leukemia (AML)	2
2	Completed	Treatment	Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome / Adult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Untreated Adult Acute Myeloid Leukemia	1
2	Completed	Treatment	Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Untreated Adult Acute Myeloid Leukemia	1
2	Completed	Treatment	Adenocarcinoma of the Pancreas / Recurrent Pancreatic Cancer / Stage IV Pancreatic Cancer	1
2	Completed	Treatment	Adenocarcinomas of the Gastroesophageal Junction / Advanced Gastric Cancer / Diffuse Adenocarcinoma of the Stomach / Intestinal Adenocarcinoma of the Stomach / Mixed Adenocarcinoma of the Stomach / Recurrent Gastric Cancer / Stage IIIA Gastric Cancer / Stage IIIB Gastric Cancer / Stage IIIC Gastric Cancer	1
2	Completed	Treatment	Adult Acute Basophilic Leukemia / Adult Acute Eosinophilic Leukemia / Adult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Secondary Acute Myeloid Leukemia (Secondary AML, sAML) / Untreated Adult Acute Myeloid Leukemia	1
2	Completed	Treatment	Adult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Recurrent Adult Acute Myeloid Leukemia	1
2	Completed	Treatment	B-Cell Chronic Lymphocytic Leukemia / Chronic Lymphocytic Leukemia (CLL) - Refractory / Stage I Chronic Lymphocytic Leukemia / Stage II Chronic Lymphocytic Leukemia / Stage III Chronic Lymphocytic Leukemia / Stage IV Chronic Lymphocytic Leukemia	1
2	Completed	Treatment	Chronic Lymphocytic Leukaemia (CLL)	1
2	Completed	Treatment	Endometrial Cancer	1

Pharmacoeconomics

Manufacturers: Not Available
Packagers: Not Available
Dosage Forms: Not Available
Prices: Not Available
Patents: Not Available

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.094 mg/mL	ALOGPS
logP	2.81	ALOGPS
logP	2.48	ChemAxon
logS	-3.6	ALOGPS
pKa (Strongest Acidic)	6.71	ChemAxon
pKa (Strongest Basic)	7.36	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	6	ChemAxon
Hydrogen Donor Count	3	ChemAxon
Polar Surface Area	90.23 Å²	ChemAxon
Rotatable Bond Count	2	ChemAxon
Refractivity	107.74 m³·mol^-1	ChemAxon
Polarizability	40.85 Å³	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.9932
Blood Brain Barrier	-	0.557
Caco-2 permeable	+	0.6029
P-glycoprotein substrate	Substrate	0.9095
P-glycoprotein inhibitor I	Non-inhibitor	0.8213
P-glycoprotein inhibitor II	Non-inhibitor	0.7929
Renal organic cation transporter	Non-inhibitor	0.6429
CYP450 2C9 substrate	Non-substrate	0.7975
CYP450 2D6 substrate	Non-substrate	0.6651
CYP450 3A4 substrate	Substrate	0.6517
CYP450 1A2 substrate	Non-inhibitor	0.6845
CYP450 2C9 inhibitor	Non-inhibitor	0.8621
CYP450 2D6 inhibitor	Non-inhibitor	0.7374
CYP450 2C19 inhibitor	Non-inhibitor	0.7358
CYP450 3A4 inhibitor	Non-inhibitor	0.9008
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.8937
Ames test	Non AMES toxic	0.7686
Carcinogenicity	Non-carcinogens	0.9375
Biodegradation	Not ready biodegradable	0.9923
Rat acute toxicity	2.7659 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.5312
hERG inhibition (predictor II)	Non-inhibitor	0.715

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Targets

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	170	N/A	N/A	16584130
IC 50 (nM)	170	8	30	11063609 / 12824044
IC 50 (nM)	220	7.2	37	11960485
IC 50 (nM)	40	N/A	N/A	18469809
IC 50 (nM)	960	7	22	15780638
Kd (nM)	550	N/A	N/A	18183025 / 22037378
Ki (nM)	190	N/A	N/A	23252711

Details1. Cyclin-dependent kinase 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Metal ion binding
Specific Function: Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, N...
Gene Name: CDK2
Uniprot ID: P24941
Uniprot Name: Cyclin-dependent kinase 2
Molecular Weight: 33929.215 Da

References

Zvelebil MJ: Flavopiridol Hoechst AG. IDrugs. 1998 Jun;1(2):241-6. [PubMed:18465538]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	170	7	30	15689157
Kd (nM)	110	N/A	N/A	18183025 / 22037378
Kd (nM)	43	N/A	N/A	15711537

Details2. Cyclin-dependent kinase 5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Tau-protein kinase activity
Specific Function: Proline-directed serine/threonine-protein kinase essential for neuronal cell cycle arrest and differentiation and may be involved in apoptotic cell death in neuronal diseases by triggering abortive...
Gene Name: CDK5
Uniprot ID: Q00535
Uniprot Name: Cyclin-dependent-like kinase 5
Molecular Weight: 33304.125 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	20	N/A	N/A	18469809
Kd (nM)	6.4	N/A	N/A	18183025 / 22037378
Ki (nM)	3	N/A	N/A	23252711

Details3. Cyclin-dependent kinase 9

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Transcription regulatory region dna binding
Specific Function: Protein kinase involved in the regulation of transcription. Member of the cyclin-dependent kinase pair (CDK9/cyclin-T) complex, also called positive transcription elongation factor b (P-TEFb), whic...
Gene Name: CDK9
Uniprot ID: P50750
Uniprot Name: Cyclin-dependent kinase 9
Molecular Weight: 42777.155 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	200	N/A	N/A	10843211
IC 50 (nM)	200	7.5	22	15780638
IC 50 (nM)	30	N/A	N/A	20638755
IC 50 (nM)	30	8	30	11063609 / 12190313 / 12824044
IC 50 (nM)	400	N/A	N/A	15559249

Details4. Cyclin-dependent kinase 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Rna polymerase ii carboxy-terminal domain kinase activity
Specific Function: Plays a key role in the control of the eukaryotic cell cycle by modulating the centrosome cycle as well as mitotic onset; promotes G2-M transition, and regulates G1 progress and G1-S transition via...
Gene Name: CDK1
Uniprot ID: P06493
Uniprot Name: Cyclin-dependent kinase 1
Molecular Weight: 34095.14 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	80	7	30	15689157

Details5. Cyclin-dependent kinase 6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Cyclin-dependent protein serine/threonine kinase activity
Specific Function: Serine/threonine-protein kinase involved in the control of the cell cycle and differentiation; promotes G1/S transition. Phosphorylates pRB/RB1 and NPM1. Interacts with D-type G1 cyclins during int...
Gene Name: CDK6
Uniprot ID: Q00534
Uniprot Name: Cyclin-dependent kinase 6
Molecular Weight: 36938.025 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	>10000	N/A	N/A	18183025
Kd (nM)	1200	N/A	N/A	22037378
Kd (nM)	1400	N/A	N/A	18183025 / 22037378
Kd (nM)	1600	N/A	N/A	22037378
Kd (nM)	1700	N/A	N/A	22037378
Kd (nM)	2200	N/A	N/A	22037378
Kd (nM)	2300	N/A	N/A	18183025 / 22037378
Kd (nM)	3000	N/A	N/A	22037378
Kd (nM)	3700	N/A	N/A	22037378
Kd (nM)	4000	N/A	N/A	22037378
Kd (nM)	520	N/A	N/A	22037378
Kd (nM)	750	N/A	N/A	22037378

Details6. Epidermal growth factor receptor

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Ubiquitin protein ligase binding
Specific Function: Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TG...
Gene Name: EGFR
Uniprot ID: P00533
Uniprot Name: Epidermal growth factor receptor
Molecular Weight: 134276.185 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	100	N/A	N/A	16584130
IC 50 (nM)	100	7.2	30	10969976
IC 50 (nM)	100	8	30	11063609 / 12824044
IC 50 (nM)	180	7	22	15780638
IC 50 (nM)	400	7.2	37	11960485
Kd (nM)	3.3	N/A	N/A	22037378
Kd (nM)	9	N/A	N/A	22037378

Details7. Cyclin-dependent kinase 4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Cyclin-dependent protein serine/threonine kinase regulator activity
Specific Function: Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S tra...
Gene Name: CDK4
Uniprot ID: P11802
Uniprot Name: Cyclin-dependent kinase 4
Molecular Weight: 33729.55 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	120	N/A	N/A	18183025 / 22037378

Details8. Cyclin-dependent kinase 8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Ubiquitin protein ligase activity
Specific Function: Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from ...
Gene Name: CDK8
Uniprot ID: P49336
Uniprot Name: Cyclin-dependent kinase 8
Molecular Weight: 53283.335 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	875	N/A	N/A	18469809
Kd (nM)	23	N/A	N/A	18183025 / 22037378

Details9. Cyclin-dependent kinase 7

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Transcription coactivator activity
Specific Function: Serine/threonine kinase involved in cell cycle control and in RNA polymerase II-mediated RNA transcription. Cyclin-dependent kinases (CDKs) are activated by the binding to a cyclin and mediate the ...
Gene Name: CDK7
Uniprot ID: P50613
Uniprot Name: Cyclin-dependent kinase 7
Molecular Weight: 39038.005 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	1000	N/A	N/A	15214781

Details10. Glycogen phosphorylase, muscle form

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Pyridoxal phosphate binding
Specific Function: Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known ...
Gene Name: PYGM
Uniprot ID: P11217
Uniprot Name: Glycogen phosphorylase, muscle form
Molecular Weight: 97091.265 Da

References

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Details11. Glycogen phosphorylase, brain form

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Pyridoxal phosphate binding
Specific Function: Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known ...
Gene Name: PYGB
Uniprot ID: P11216
Uniprot Name: Glycogen phosphorylase, brain form
Molecular Weight: 96695.18 Da

References

Kaiser A, Nishi K, Gorin FA, Walsh DA, Bradbury EM, Schnier JB: The cyclin-dependent kinase (CDK) inhibitor flavopiridol inhibits glycogen phosphorylase. Arch Biochem Biophys. 2001 Feb 15;386(2):179-87. [PubMed:11368340]

Details12. Glycogen phosphorylase, liver form

Kind: Protein
Organism: Humans
Pharmacological action: Unknown

General Function: Vitamin binding
Specific Function: Phosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known ...
Gene Name: PYGL
Uniprot ID: P06737
Uniprot Name: Glycogen phosphorylase, liver form
Molecular Weight: 97147.82 Da

References

Kaiser A, Nishi K, Gorin FA, Walsh DA, Bradbury EM, Schnier JB: The cyclin-dependent kinase (CDK) inhibitor flavopiridol inhibits glycogen phosphorylase. Arch Biochem Biophys. 2001 Feb 15;386(2):179-87. [PubMed:11368340]

Enzymes

Details1. UDP-glucuronosyltransferase 1-1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Steroid binding
Specific Function: UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name: UGT1A1
Uniprot ID: P22309
Uniprot Name: UDP-glucuronosyltransferase 1-1
Molecular Weight: 59590.91 Da

References

Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [PubMed:15304429]

Transporters

Details1. ATP-binding cassette sub-family G member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name: ABCG2
Uniprot ID: Q9UNQ0
Uniprot Name: ATP-binding cassette sub-family G member 2
Molecular Weight: 72313.47 Da

References

Nakanishi T, Karp JE, Tan M, Doyle LA, Peters T, Yang W, Wei D, Ross DD: Quantitative analysis of breast cancer resistance protein and cellular resistance to flavopiridol in acute leukemia patients. Clin Cancer Res. 2003 Aug 15;9(9):3320-8. [PubMed:12960118]
Nakanishi T, Doyle LA, Hassel B, Wei Y, Bauer KS, Wu S, Pumplin DW, Fang HB, Ross DD: Functional characterization of human breast cancer resistance protein (BCRP, ABCG2) expressed in the oocytes of Xenopus laevis. Mol Pharmacol. 2003 Dec;64(6):1452-62. [PubMed:14645676]
Shi Z, Parmar S, Peng XX, Shen T, Robey RW, Bates SE, Fu LW, Shao Y, Chen YM, Zang F, Chen ZS: The epidermal growth factor tyrosine kinase inhibitor AG1478 and erlotinib reverse ABCG2-mediated drug resistance. Oncol Rep. 2009 Feb;21(2):483-9. [PubMed:19148526]

Drug created on June 13, 2005 07:24 / Updated on November 02, 2020 21:00

Alvocidib

Identification

Structure for Alvocidib (DB03496)

Pharmacology

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Enzymes

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