LY-3177833

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

一种有效的选择性 CDC7 抑制剂，IC50 为 3.3 nM。

A potent and selective CDC7 inhibitor with IC50 of 3.3 nM.(In Vitro):LY3177833 (10 μM; 4 days) increases SA-β-gal content in Hep3B cells.(In Vivo):LY3177833 (Example 4; 10.4-31.2 mg/kg; oral gavage; twice a day; for 2 weeks; female athymic Balb/c nude mice with SW620 cells) treatment causes significant tumor regression in a dose-dependent manner. Also, no significant tumor growth is observed for 2 weeks after dosing cessation.

LY3177833 (10 μM; 4 days) increases SA-β-gal content in Hep3B cells.Western Blot Analysis Cell Line:Hep3B cells Concentration:10 μM Incubation Time:4 days Result:Increased the expression of human SA-β-gal.

LY3177833 (Example 4; 10.4-31.2 mg/kg; oral gavage; twice a day; for 2 weeks; female athymic Balb/c nude mice with SW620 cells) treatment causes significant tumor regression in a dose-dependent manner. Also, no significant tumor growth is observed for 2 weeks after dosing cessation. Animal Model:Female athymic Balb/c nude mice (5-6 weeks old) with SW620 cells Dosage:10.4 mg/kg, 20.8 mg/kg and 31.2 mg/kg Administration:Oral gavage; twice a day for 2 weeks Result:Showed dose dependent antitumor activity in SW620 mouse xenograft tumor model.

LY3177833

Angiogenesis

CDK

CDK

Cancer

——

1627696-51-8

309.2978

C16H12FN5O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C1N[C@@](C)(C2=NC=NC=C2F)C3=C1C=C(C4=CNN=C4)C=C3

1H-Isoindol-1-one, 3-(5-fluoro-4-pyrimidinyl)-2,3-dihydro-3-methyl-6-(1H-pyrazol-4-yl)-, (3R)-

(-20℃)

With Ice Pack

≥ 2 years