Chemical Name: N-[(5,6-Dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methylpyrazol-4-yl)-2-morpholin-4-ylpurin-6-amine
CDK12/13 inhibitor
Molekulargewicht:
499.36
Reinheit:
98% by TLC NMR (Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[2387704-62-1]
Formel:
C21H20Cl2N10O
Anwendungsbeschreibung:
SR-4835 is a potent and selective inhibitor of cyclin-dependent kinases 12 and 13 (KD50s: CDK12 = 98 nM, CDK13 = 4.9 nM).1 It displayed efficacy against multiple triple-negative breast cancer cell lines (EC50s: MDA-MB-231 15.5 nM, MDA-MB-468 22.1 nM, HS578T 19.9 nM, MDA-MB-436 24.9 nM). Inhibition of CDK12/13 with SR-4835 resulted in down-regulation of multiple DNA damage response genes and caused increased DNA damage and apoptosis. SR-4835 acted synergistically with DNA-damaging agents and PARP inhibitors to cause triple-negative breast cancer cell death.1,2 It acted synergistically with PD-1 blockade to provide a durable immune-mediated antitumor response in a syngeneic breast cancer mouse model.3 SR-4835 has been found to act as a molecular glue that promotes cyclin K degradation.4 Inhibition of CDK12 with SR-4835 suppressed tumor initiation and growth in a colorectal cancer mouse model and impaired liver metastasis of colorectal cancer cells while also diminishing cancer stem cell traits through ß-catenin pathway activation.5
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