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Cat. No. Product Name CAS No. Information
PC-60310

GNE-900

1200126-26-6

GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM; displays >300-fold selectivity over Aurora, PLK, CDK1/2) and ChK2; abrogates DNA damage-induced S and G2–M checkpoints (EC50=61.8 nM in H-29 cells), and exacerbates DNA double-strand breaks (DSB) to induce cell death, accelerates the demise of damaged HCT-116 colorectal cancer cells in a p53-dependent manner in vitro; potentiates the efficacy of gemcitabine in tumor xenografts.

PC-60276

GDC-0575

1196541-47-5

GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM; enhances the killing of primary AML cells ex vivo by inducing apoptosis combined with AraC, blocks the activation of CHK1 induced by AraC via decrease in the level of Tyr15-phosphorylated CDK2 at 100 nM in AML cells.

Blood Cancer

Phase 1 Clinical

PC-42769

AZD-7762

860352-01-8

AZD-7762 (AZD7762) is a potent and selective inhibitor of Chk1/2 with IC50 of 5 nM; shows less potent against CAM, Yes, Fyn, Lyn, Hck and Lck; enhances the radiosensitivity of mutated p53 tumor cell lines and HT29 xenografts.

Solid Tumors

Phase 1 Discontinued

PC-35602

PF-00477736

952021-60-2 PF-00477736 (PF-477736) is a potent, selective, ATP-competitive inhibitor of Chk1 with Ki of 0.49 nM, also inhibits Chk2 (Ki=47 nM) and poorly inhibits CDK1 activity (Ki=9.9 uM); displays <100-fold selectivity over VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret, and Yes in a panel of >100 protein kinases; abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin; enhances the antitumor activity of gemcitabine in a dose-dependent manner in xenografts.

Solid Tumors

Phase 1 Discontinued

PC-43443

CHIR-124

405168-58-3 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.
PC-63128

BAY-1816032

1891087-61-8 BAY-1816032 is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases; abrogates nocodazole-induced Thr-120 phosphorylation of the major BUB1 target protein histone H2A in HeLa cells with IC50 of 29 nM, induces lagging chromosomes and mitotic delay, inhibits proliferation of various tumor cell lines with mean IC50 of 1.4 uM; demonstrates synergy or additivity with paclitaxel or docetaxel both in vitro and in vivo.
PC-63043

SAR-020106

1184843-57-9 SAR-020106 (SAR-20106) is a potent and selective CHK1 inhibitor with IC50 of 13 nM, with high selectivity over CHK2 (IC50>100 uM); inhibits HT29 cells with IC50 of 0.53 uM in SRB cytotoxicity assay; inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo.

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