Dalpiciclib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Dalpiciclib 是一种高度选择性、口服生物可利用且效力相当的 CDK4 和 CKD6 抑制剂，IC50 为 12.4纳米和 9.9分别为nM。

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.

Dalpiciclib (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner.Dalpiciclib (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines. Cell Proliferation AssayCell 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.Cell Viability Assay Cell Line:MCF7, MCF7/TR, BT-474/T cell lines Concentration:0-10 μM Incubation Time:6 ?days Result:Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC50 values of 229.5, 115.4 and 210.7 nM, respectively.

Dalpiciclib (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts.Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts.Dalpiciclib (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models . Animal Model:NOD/SCID mice (ESCC PDXs models) Dosage:150 mg/kg Administration:Oral gavage; 150 mg/kg; once weekly; 3 weeks Result:Suppressed the growth of tumor.Animal Model:5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG Dosage:37.5 mg/kg, 75 mg/kg, 150 mg/kg Administration:Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days Result:Caused regression of all tumor xenografts at the highest dose tested.

SHR-6390

Angiogenesis

CDK

Ryanodine receptor|insecticide

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1637781-04-4

446.54

C25H30N6O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (111.97 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years