LY3143921

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

LY3143921 (LY-3143921) 是一种口服有效的 Cdc7 激酶抑制剂的选择性抑制剂，抑制 CDC7/DBF4 I 和 pMCM2 (S53)，IC50 值分别为 3.3 nM 和 290 nM。

LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively.Solid Tumors Phase 1 Clinical.

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 cellsDosage:10.4 mg/kg, 20.8 mg/kg and 31.2 mg/kg Administration:Oral gavage; twice a day for 2 weeksResult:Showed dose dependent antitumor activity in SW620 mouse xenograft tumor model.

LY-3143921 | LY 3143921

Cell Cycle/DNA Damage

CDK

CDK

Cancer

Solid Tumors

1627696-53-0

327.319

C16H14FN5O2

>98% (HPLC)

——

CC1(C2=C(C=C(C=C2)C3=CNN=C3)C(=O)N1)C4=NC=NC=C4F.O

(3R)-3-(5-Fluoro-4-pyrimidinyl)-2,3-dihydro-3-methyl-6-(1H-pyrazol-4-yl)-1H-isoindol-1-one hydrate

(-20℃)

With Ice Pack

≥ 2 years