SR-4835, CDK12/13 inhibitor (TBI4864)

Description

Product Details

Formal Name: N-[(5,6-Dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methylpyrazol-4-yl)-2-morpholin-4-ylpurin-6-amine

Molecular Formula: C₂₁H₂₀Cl₂N₁₀O

Formula Weight: 499.4

CAS Number: 2387704-62-1

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml).

Storage: -20°C

Stability: ≥ 2 years

Applications

CDK12/13 inhibitor

Functions

Potent and selective inhibitor of cyclin-dependent kinases 12 and 13 (KD₅₀s: CDK12 = 98 nM, CDK13 = 4.9 nM). 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. Acted synergistically with DNA-damaging agents and PARP inhibitors to cause triple-negative breast cancer cell death. It acted synergistically with PD-1 blockade to provide a durable immune-mediated antitumor response in a syngeneic breast cancer mouse model. Has been found to act as a molecular glue that promotes cyclin K degradation. 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.

Application Procedures

First dissolved in DMSO (>25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4864_SR-4835_datasheet

MSDS:

TBI4864_SR-4835HCl_MSDS

Research use only.