Riviciclib hydrochloride
P276-00
CAS: 920113-03-7
Molecular Formula: C21H21Cl2NO5
Riviciclib hydrochloride - Names and Identifiers
| Name | P276-00 |
| Synonyms | P276 CS-996 P276-00 Riviciclib HCl Riviciclib hydrochloride RIVICICLIB HYDROCHLORIDE (P276-00) |
| CAS | 920113-03-7 |
Riviciclib hydrochloride - Physico-chemical Properties
| Molecular Formula | C21H21Cl2NO5 |
| Molar Mass | 438.3 |
| Storage Condition | -20℃ |
| Use | P276-00 is a novel CDK1,CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM respectively. Phase 2/3. |
| In vitro study | P276-00 acting on Cdk4-D1 is 40 times more selective than acting on Cdk2-E. P276-00 has potent antiproliferative effects on a variety of human cancer cell lines, including HCT-116, U2OS, H-460, HL-60, HT-29, SiHa, MCF-7, Colo-205, SW-480, PC-3, Caco2, T-24, the IC50 is 300 to 800 nmol/L and is highly selective for cancer cells over normal fibroblasts. P276-00 can downregulate cyclin D1 and Cdk4 in an ATP-competitive manner, reducing Cdk4 specific pRb Ser780 phosphorylation. P276-00 also induces apoptosis by activating cell caspase-3 activity and DNA ladder formation. |
| In vivo study | P276-00 treatment of colon cancer (CA-51) in mice with daily intraperitoneal injection of 50 mg/kg for 20 days significantly induced inhibition of tumor growth. P276-00 treatment of a mouse lung cancer model (Lewis lung cancer) at a higher dose of 60 mg/kg (30 mg/kg twice daily), every other day for 7 days, significantly inhibited tumor growth. P276-00 also inhibits the growth of human colon cancer HCT-116 xenografts and human non-small cell lung cancer H-460 xenografts. Efficacy studies indicated that the maximum tolerated dose of P276-00 was 78 mg/kg/d. |
Riviciclib hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.282 ml | 11.408 ml | 22.815 ml |
| 5 mM | 0.456 ml | 2.282 ml | 4.563 ml |
| 10 mM | 0.228 ml | 1.141 ml | 2.282 ml |
| 5 mM | 0.046 ml | 0.228 ml | 0.456 ml |
Last Update：2024-01-02 23:10:35
Riviciclib hydrochloride - Reference Information
| biological activity | P276-00 is a novel CDK1,CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM. Phase 2/3. Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3. |
| Target | Value |
| CDK9/CyclinT1 | 20 nM |
| CDK4/CyclinD1 | 63 nM |
| CDK1/CyclinB () | 79 nM |
| CDK2/CyclinA | 224 nM |
| CDK6/CyclinD3 | 396 nM |
Last Update：2024-04-09 19:05:17
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CAS: 920113-03-7
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CAS: 920113-03-7
Tel: 18301782025
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Mobile: 18021002903
QQ: 3008007409
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