CHIR-124

Research use only, not for human use.

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM.

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2; displays 500- to 5,000-fold less active against other cell cycle kinases, such as CDK2/cyclin A , Cdc2/cyclin B, and CDK4/cyclin D; also potently inhibits PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM; interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines, abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells, also restores the level of cdc25A protein; potentiates the growth inhibitory effects of irinotecan in breast cancer xenograft models.

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CHIR124 | CHIR 124

Angiogenesis

Chk

Chk1|FLT3|Fyn|GSK-3|PDGFR

Cancer

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405168-58-3

419.91

C23H22ClN5O

>98% (HPLC)

DMSO: 14 mg/mL

O=C1NC2=C(C=C(Cl)C=C2)C(N[C@@H]3C[N@]4CC[C@]3([H])CC4)=C1C5=NC6=CC=CC=C6N5

2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-

(-20℃)

With Ice Pack

≥ 2 years