784211-09-2
784211-09-2 structure
- Name: RGB-286147
- Chemical Name: 1-(2,6-dichlorophenyl)-6-[[4-(2-hydroxyethoxy)phenyl]methyl]-3-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-4-one
- CAS Number: 784211-09-2
- Molecular Formula: C23H22Cl2N4O3
- Molecular Weight: 473.35200
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2016-10-02 04:15:05
- Modify Date: 2024-01-11 13:18:11
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RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with 50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1].
| Name | 1-(2,6-dichlorophenyl)-6-[[4-(2-hydroxyethoxy)phenyl]methyl]-3-propan-2-yl-2H-pyrazolo[3,4-d]pyrimidin-4-one |
|---|---|
| Synonyms |
Cdk/Crk Inhibitor
HMS3229E20 |
| Description | RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with 50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity[1]. |
|---|---|
| Related Catalog | |
| Target |
CDK1/cyclinB:48 nM (IC50) CDK2/E:15 nM (IC50) CDK4/D1:839 nM (IC50) cdk6/cyclin D3:232 nM (IC50) |
| In Vitro | RGB-286147（50-100 nM；24-48 小时）在 G1 期诱导细胞周期停滞，显着抑制 DNA 复制，并诱导 HCT116 细胞凋亡[1]。 RGB-286147（100 nM；48 小时）导致 HCT116 细胞中 PARP 的蛋白水解裂解[1]。 RGB-286147（24-72 小时）在 HCT116 细胞中表现出有效且不可逆的细胞杀伤活性。RGB-286147 抑制集落形成的 IC50 值为 57 nM[1]。 RGB-286147（48 小时）表现出广泛的抗肿瘤活性，对于 60 种致瘤细胞系，平均 GI50 值 <10 nM。并且还抑制非循环 HCT116 细胞的生长，IC50 值为 40 nM[1]。 Cell Cycle Analysis[1] Cell Line: HCT116 cells Concentration: 50 nM and 100 nM Incubation Time: 24 or 48 hr Result: Caused a marked inhibition of DNA replication and induced cell cycle arrest. Western Blot Analysis[1] Cell Line: HCT116 cells Concentration: 100 nM Incubation Time: 48 hr Result: Resulted in proteolytic cleavage of PARP. |
| References |
| Molecular Formula | C23H22Cl2N4O3 |
|---|---|
| Molecular Weight | 473.35200 |
| Exact Mass | 472.10700 |
| PSA | 93.03000 |
| LogP | 4.50090 |