SR-4835
Product Sizes
5 mg
£163.00
10-4864-5MG
25 mg
£267.00
10-4864-25MG
About this Product
- SKU:
- 10-4864
- Additional Names:
- CDK12/13 inhibitor, N-[(5,6-Dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methylpyrazol-4-yl)-2-morpholin-4-ylpurin-6-amine
- CAS Number:
- 2387704-62-1
- Extra Details:
- 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 B Beta-catenin pathway activation.5
- Immunogen:
- Kinase|Molecular glue
- Molecular Weight:
- 499.36
- Physical State:
- Solid
- Purity:
- 98%
- Shipping Conditions:
- Ambient
- Storage Conditions:
- -20[o]C
- Supplier:
- Focus Biomolecules
- Type:
- Proteins, Peptides, Small Molecules & Other Biomolecules: Inhibitors
