SR-4835 是有效,高选择性和 ATP 竞争性的 CDK12/CDK13 双重抑制剂。 SR-4835 与破坏 DNA 的化学疗法和 PARP 抑制剂协同作用,并引起三阴性乳腺癌 (TNBC) 细胞凋亡。 Information SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. Targets CDK13 (Cell-free assay); CDK12 (Cell-free assay); CDK12 (Cell-free assay) 4.9 nM; 98 nM(Kd); 99 nM In vitro SR-4835 is a selective, potent dual inhibitor of CDK12 and CDK13, suppressing expression of DDR proteins. CDK12/CDK13 inhibition synergizes with DNA-damaging agents or PARP inhibition to trigger TNBC cell death. In vivo SR-4835 has potent in vivo anti-TNBC activity and augments the anti-cancer activity of cisplatin, irinotecan, and olaparib, which are standard-of-care therapeutics for TNBC. SR-4835 is well tolerated in mice after long-term dosing. SR-4835 cooperates with DNA-damaging chemotherapeutics. Cell Research(from reference) Cell lines:Human: MDA-MB-231, MDA-MB-436, HS578T, MDA-MB-468, FHC Concentrations:10-90 nM, 0.4-10 μM Incubation Time:4 h, 6 h, 72 h
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SR-4835
Dangerous GoodsCAS number:2387704-62-1 molecular formula:C21H2OCl2N10O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | 9H-Purin-6-amine,N-[(5,6-dichloro-1H-benzimidazol-2-yl)methyl]-9-(1-methyl-1H-pyrazol-4-yl)-2-(4-morpholinyl)- | ||
| CAS number | 2387704-62-1 | molecular formula | C21H2OCl2N10O |
| molecular weight | 499.36 g/mol | Exact mass | - |
| PSA | 115.000 Ų | logp | 3.538 |
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Safety information
pictogram:
GHS07
Signal word:
Warning
Hazard Statement:
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures:
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染:用水充分清洗。 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。
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