SF1126
Identification
- Generic Name
- SF1126
- DrugBank Accession Number
- DB05210
- Background
SF1126 is an integrin-targeted PI3 kinase inhibitor.
- Type
- Small Molecule
- Groups
- Investigational
- Synonyms
- SF 1126
- SF-1126
Pharmacology
- Indication
For the treatment of various forms of cancer.
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- Pharmacodynamics
SF1126 is a covalent conjugate of LY294002 that contains a peptide-based targeting group to help increase the localization of the drug in the neovascular component supporting tumor growth. SF1126 is a highly water soluble solid which aids its administration via i.v. or s.c. injections. In vivo it converts spontaneously at physiological pH to LY294002 in a way that is well tolerated in mice, rats, and dogs. SF1126 has been evaluated in numerous animal tumor models showing good tumor inhibition or tumor regression.
- Mechanism of action
SF1126 is a small molecule conjugate containing a pan-PI3K inhibitor that selectively inhibits all PI3K class IA isoforms and other key members of the PI3K superfamily, including DNA-PK and mTOR. A major factor in tumor resistance to approved chemotherapy agents is thought to be the activation of the PI3K/PTEN pathway. As a result, it is thought that inhibiting this pathway, via SF1126, could cause the resetting of sensitivity to approved agents and exhibit synergistic anticancer effects.
Target Actions Organism UPhosphatidylinositol 3-kinase regulatory subunit alpha Not Available Humans UPhosphatidylinositol 3-kinase regulatory subunit beta Not Available Humans UPhosphatidylinositol 3-kinase regulatory subunit gamma Not Available Humans UDNA-dependent protein kinase catalytic subunit Not Available Humans USerine/threonine-protein kinase mTOR 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
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.Not Available
- Food Interactions
- Not Available
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- DL0Q912033
- CAS number
- Not Available
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Not Available
- External Links
- PubChem Substance
- 347910028
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 2 Terminated Treatment Squamous Cell Carcinoma Metastatic in the Neck With Occult Primary 1 1 Completed Treatment Advanced or Metastatic Solid Tumor / Cancer / Solid Cancers 1 1 Terminated Treatment Advanced Hepatocellular Carcinoma (HCC) 1 1 Terminated Treatment Neuroblastoma (NB) 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
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Transmembrane receptor protein tyrosine kinase adaptor activity
- Specific Function
- Binds to activated (phosphorylated) protein-Tyr kinases, through its SH2 domain, and acts as an adapter, mediating the association of the p110 catalytic unit to the plasma membrane. Necessary for t...
- Gene Name
- PIK3R1
- Uniprot ID
- P27986
- Uniprot Name
- Phosphatidylinositol 3-kinase regulatory subunit alpha
- Molecular Weight
- 83597.675 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Receptor tyrosine kinase binding
- Specific Function
- Regulatory subunit of phosphoinositide-3-kinase (PI3K), a kinase that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3...
- Gene Name
- PIK3R2
- Uniprot ID
- O00459
- Uniprot Name
- Phosphatidylinositol 3-kinase regulatory subunit beta
- Molecular Weight
- 81544.505 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- 1-phosphatidylinositol-3-kinase regulator activity
- Specific Function
- Binds to activated (phosphorylated) protein-tyrosine kinases through its SH2 domain and regulates their kinase activity. During insulin stimulation, it also binds to IRS-1.
- Gene Name
- PIK3R3
- Uniprot ID
- Q92569
- Uniprot Name
- Phosphatidylinositol 3-kinase regulatory subunit gamma
- Molecular Weight
- 54448.0 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Transcription factor binding
- Specific Function
- Serine/threonine-protein kinase that acts as a molecular sensor for DNA damage. Involved in DNA non-homologous end joining (NHEJ) required for double-strand break (DSB) repair and V(D)J recombinati...
- Gene Name
- PRKDC
- Uniprot ID
- P78527
- Uniprot Name
- DNA-dependent protein kinase catalytic subunit
- Molecular Weight
- 469084.155 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Tfiiic-class transcription factor binding
- Specific Function
- Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly...
- Gene Name
- MTOR
- Uniprot ID
- P42345
- Uniprot Name
- Serine/threonine-protein kinase mTOR
- Molecular Weight
- 288889.05 Da
Drug created at October 21, 2007 22:24 / Updated at July 18, 2023 22:56