Dalpiciclib

Research use only, not for human use.

Dalpiciclib 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 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.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.(In Vivo):Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts.

SHR-6390

Angiogenesis

CDK

Ryanodine receptor;insecticide

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1637781-04-4

446.5

C25H30N6O2

>98% (HPLC)

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CC(C1=C(C)c2cnc(Nc3ncc(C4CCNCC4)cc3)nc2N(C2CCCC2)C1=O)=O

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(-20℃)

With Ice Pack

≥ 2 years