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Cat. No. Product Name CAS No. Information
PC-62560

AS 703569

871357-89-0

Cenisertib (AS 703569;R763) is a novel potent, orally available inhibitor of Aurora kinases, exhibits signifficant anti-proliferative activity against a wide range of tumor cells both in vitro and in vivo (A549 EC50=9 nM); demonstrates marked inhibition of tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

Solid Tumors

Phase 1 Discontinued

PC-42409

Tozasertib

639089-54-6

Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively; also inhibits the imatinib-resistant ABL(T315I) kinase with Kd of 5 nM, displays >100-fold selectivity for the Aurora-A kinase over 55 other kinases with the only exception FLT-3 (Ki=30 nM); blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types; causes profound inhibition of tumor growth in a variety of in vivo xenograft models.

Blood Cancer

Discontinued

PC-35756

LY3295668

1919888-06-4 LY3295668 (LY-3295668, AK-01) is a novel potent, highly selective, orally active Aurora-A kinase inhibitor with Ki of 0.8 nM, H446 AurA auto-P IC50 of 0.6 nM; displays >1000-fold selectivity over Aur-B, 5/386 kinases were potently inhibited by LY3295668 (<10 nM) and none of these kinases overlapped with targets of the other AurAi (MK5108, alisertib), and no inhibition of SYK; LY3295668 is cytotoxic to RB1 mutant cancer cancaer cells (NCI-H446 cell IC50=0.752 uM), causes durable regression of RB1mut tumor xenografts.

Solid Tumors

Phase 2 Clinical

PC-43432

AMG-900

945595-80-2 AMG-900 (AMG900) is a potent, highly selective, orally bioavailable pan-Aurora kinase inhibitor with IC50 of 5, 4 and 1 nM for Aurora A, B and C, respectively; displays excellent specificity in a panel of 26 kinases with exception of p38α and TYK2 (IC50=53 and 220 nM), also exhibits high affinity (Kd< 50 nM) with DDR1, DDR2, and LTK receptor tyrosine kinases; blocks the proliferation of multiple human tumor cell lines including cell lines resistant to paclitaxel, AZD1152, MK-0457, and PHA-739358 with IC50 of 0.7-5.3 nM; blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibits the growth of HCT116 tumor xenografts.

Blood Cancer

Phase 1 Clinical

PC-43431

MK-5108

1010085-13-8 MK-5108 (VX-689) is a potent, highly selective Aurora-A kinase inhibitor with IC50 of 0.064 nM, displays robust selectivity against Aurora-B (220-fold) and Aurora-C (190-fold) in the biochemical assays; also exhibits high selectivity for Aurora-A over a panel of 233 kinases, only one kinase (TrkA) with <100-fold selectivity; inhibits the growth of multiple human cancer cell lines in vitro and in human cancer xenograft models; MK-5108 significantly enhanced the efficacy of docetaxel without increasing its toxicity.

Solid Tumors

Phase 1 Clinical

PC-63253

BI 831266

958227-46-8 BI 831266 is a potent, selective inhibitor of Aurora kinase B (AURKB) with IC50 of binding IC50 of 42 nM; inhibits the proliferation of human non-small cell lung cancer (NSCLC), pancreatic cancer, and prostate cancer cell lines (H460 tumor cell proliferation inhibition IC50=11 nM); causes tumor regression and growth inhibition in in murine xenograft tumor models (HCT 116 colon carcinoma, BxPC3 pancreatic adenocarcinoma, and NCI-H460 NSCLC).

Solid Tumors

Phase 1 Clinical

PC-42348

ZM-447439

331771-20-1 ZM-447439 is a potent, selective dual Aurora A and Aurora B inhibitor with IC50 of 110 and 130 nM, respectively; prevents anaplastic thyroid cancer cell growth and tumorigenicity, inhibits the growth and tumorigenicity of a panel of ATC derived cell lines (CAL-62, 8305C, 8505C and BHT-101) with IC50 of 0.5-5 uM; ZM447439-treated cells exit mitosis with normal kinetics, accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint.

Blood Cancer

Discontinued

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