1637781-04-4
1637781-04-4 structure
- Name: Dalpiciclib
- Chemical Name: Dalpiciclib
- CAS Number: 1637781-04-4
- Molecular Formula: C25H30N6O2
- Molecular Weight: 446.54
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2022-02-01 19:30:08
- Modify Date: 2024-01-09 23:32:39
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Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2].
| Name | Dalpiciclib |
|---|
| Description | Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2]. |
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| Related Catalog | |
| Target |
CDK4:12.4 nM (IC50) CDK6:9.9 nM (IC50) |
| In Vitro | Dalpiciclib (SHR-6390) (0-4 μM) inhibits cell proliferation in a dose-dependent manner[2]. Dalpiciclib (24 hours) significantly blocks phosphorylation of Rb at serine 780 in relative sensitive Eca 109 and KYSE-510 cell lines, but not in relative resistant Eca 9706 cell line.Dalpiciclib induces cell cycle arrest at G1 phase in Eca 109 and KYSE-510 cell lines[2]. Cell Proliferation Assay[2] Cell Line: Eca 109, Eca 9706, and KYSE-510 ESCC cell lines Concentration: 0-4 μM Incubation Time: 72 hours Result: Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one. |
| In Vivo | Dalpiciclib (SHR-6390) (150 mg/kg; oral gavage; weekly for 3 weeks) shows antitumor activity against ESCC xenografts[2]. Dalpiciclib combines with Paclitaxel (PTX) or Cisplatin (CDDP) offered synergistic inhibitory effects in ESCC xenografts[2]. Animal Model: NOD/SCID mice (ESCC PDXs models) [2] Dosage: 150 mg/kg Administration: Oral gavage; weekly for 3 weeks Result: The growth of tumor was significantly suppressed in SHR6390 treatment group with various suppressions. |
| References |
| Molecular Formula | C25H30N6O2 |
|---|---|
| Molecular Weight | 446.54 |