K03861

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

K03861 是一种 II 型 CDK2 抑制剂，对 CDK2(WT)、CDK2(C118L)、CDK2(A144C) 和 CDK2(C118L/A144C) 的 Kd 分别为 50 nM、18.6 nM、15.4 nM 和 9.7 nM。

AUZ454 is a potent and selective Type II FLT3 inhibitor. AUZ454 is able to override drug resistance that less potent "type I" inhibitors and "type II" first-generation FLT3 inhibitors cannot. Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule inhibitor, PKC412, targets mutant FLT3 and is currently in late-stage clinical trials. However, the identification of PKC412-resistant leukemic blast cells in the bone marrow of AML patients has propelled the development of novel and structurally distinct FLT3 inhibitors that have the potential to override drug resistance and more efficiently prevent disease progression or recurrence.

Cell Proliferation Assay Cell Line:Caki-1 and ACHN cells Concentration:10?μM; 20?μM Incubation Time:1, 2, 3, and 4?days Result:Inhibited cell proliferation in a CDK2-dependent manner.

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AUZ454 | AUZ 454 | AUZ-454 | K03861

Others

Other Targets

CDK2(A144C)| CDK2(C118L)| CDK2(C118L/A144C)| CDK2(WT)

Cancer

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853299-07-7

501.5

C24H26F3N7O2

>98% (HPLC)

DMSO : ≥ 33 mg/mL; 65.80 mM

CN1CCN(CC2=CC=C(NC(=O)NC3=CC=C(OC4=NC(N)=NC=C4)C=C3)C=C2C(F)(F)F)CC1

1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea

(-20℃)

With Ice Pack

≥ 2 years