BET bromodomain inhibitor (b)

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

CPI-0610 是一种有效、选择性和细胞活性的 BET bromodomain 抑制剂 CPI-0610 在时间分辨荧光能量转移 (TR-FRET ) 结合测定中抑制 BRD4-BD1，IC50 为 39 nM。

CPI-0610 is a potent, selective, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 with IC50 of 39 nM in time-resolved fluorescence energy transfer (TR-FRET ) binding assay.

Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest.Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours. Cell Viability Assay Cell Line:Multiple myeloma (MM) cell lines and primary MM cells Concentration:0 nM, 200 nM, 400 nM, 600 nM , 800 nM, 1000 nM, 1200 nM, or 1500 nM Incubation Time:72 huors Result:Decreased viability of MM cells in a dose-dependent manner. Cell Cycle Analysis Cell Line:INA6 and MM.1S cells Concentration:800 nM Incubation Time:72 hours Result:Indeced G1 cell cycle arrest.Apoptosis AnalysisCell Line:INA6 and MM.1S cells Concentration:800 nM Incubation Time:72 hours Result:MM cells apoptosis was increased after 72 hours.

Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals. Animal Model:MV-4-11 mouse xenograft modelDosage:30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily Administration:Oral administration; for 28 days Result:Suppressed of tumor growth, without any significant body weight loss in the animals.

CPI0610 | CPI 0610 | CPI-0610

Cell Cycle/DNA Damage

c-Myc

MYC| BRD4-BD1

Cancer

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1380087-89-7

365.81

C20H16ClN3O2

>98% (HPLC)

DMSO: 10 mM

O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3C4=C1ON=C4C

(S)-2-(6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide

(-20℃)

With Ice Pack

≥ 2 years