| Name | Dalpiciclib |
| Description | Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable, and comparable potency inhibitor of CDK4 and CKD6 with IC50s of 12.4 nM and 9.9 nM, respectively. Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest. |
| In vitro | Dalpiciclib inhibits cell proliferation in a dose-dependent manner following administration of 0-4 μM for 72?hours[2].In the relative sensitive Eca 109 and KYSE-510 cell lines, Dalpiciclib significantly blocks Rb phosphorylation at serine 780 after 24 hours of administration and induces cell cycle arrest but not in relative resistant Eca 9706 cell line[2]. |
| In vivo | Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts[2]. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : < 1 mg/mL (insoluble)
Methanol : 1.67 mg/mL (3.74 mM), Sonication and heating to 60°C are recommended.
1M HCl : < 1 mg/mL (insoluble)
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| Keywords | SHR6390 | SHR 6390 | MCF7/TR | MCF7 | Inhibitor | inhibit | Eca 9706 | Eca 109 | Dalpiciclib | Cyclin dependent kinase | CDK6 | CDK4 | CDK | BT-474/T | antitumor activity | and KYSE-510 ESCC |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
