Cenisertib

DB06347InvestigationalSmall molecule

Cenisertib is an aurora kinase inhibitor.

Mechanism: R763 is a highly potent and specific inhibitor of Aurora kinase, which has been shown to block proliferation and trigger apoptosis (cell death) in several tumor cell lines including cervical, colon, lung, pancreas and prostate. The over-expression of Aurora kinase can cause cells to rapidly develop an abnormal number of chromosomes. Elevated levels of Aurora kinase are frequently associated with various human cancers and inhibition of this enzyme disrupts cell division and promotes apoptosis. [Rigel Pharmaceuticals Press Release] A probable target for R763 is Aurora kinase A (serine/threonine protein kinase 6).
Curator reviewed
Primary indication: Investigated for use/treatment in solid tumors, leukemia (myeloid), myelodysplastic syndrome, and cancer/tumors (unspecified).Curator reviewed
Formula / weight: C₂₄H₃₀FN₇O · 451.55 g/mol (avg)
Code names: AS-703569 · R-763

Resolves to

Compound

Structure

InChIKeyKSOVGRCOLZZTPF-QMKUDKLTSA-NSMILES[H][C@@]12C[C@@]([H])(C=C1)[C@@H]([C@@H]2NC1=C(F)C=NC(NC2=CC=C(N3CCN(C)CC3)C(C)=C2)=N1)C(N)=O

Targets

What you can answer from here — as of August 30, 2026

2Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

3Clinical trialsPhase, status and sponsor resolved per trial

6+ReferencesStructured and connected to the statements they support

Which drugs share a target with Cenisertib, and which of those have an active Phase 3 trial?

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