Aurora Kinase

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Aurora Kinase Inhibitors (23)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3.
  • Cell Stem Cell, 2012, 11(2):179-94
  • EMBO J, 2011, 30(5):906-19
  • Nat Commun, 2013, 4:2656
S1048 VX-680 (Tozasertib, MK-0457) VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. Phase 2.
  • Cell, 2010, 142(3):444-55
  • Cell Stem Cell, 2012, 11(2):179-94
  • Curr Biol, 2011, 21(16):1356-65
S1147 Barasertib (AZD1152-HQPA) Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM, ~100 fold more selective for Aurora B over Aurora A.
  • Nat Cell Biol, 2014, 16(6):550-60
  • Curr Biol, 2011, 21(16):1356-65
  • Cancer Res, 2013, 73(20):6310-22
S1103 ZM 447439 ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
  • Cancer Res, 2013, 73(22):6722-33
  • Oncogene, 2014, 33(27):3550-60
  • Mol Cancer Ther, 2011, 10(5):784-94
S1100 MLN8054 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
  • Dev Cell, 2012, 22(1):52-63
  • J Cell Biol, 2012, 198(4):591-605
  • Cell Death Differ, 2013, 20(10):1393-403
S1107 Danusertib (PHA-739358) Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2.
  • Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1009
  • Cancer Res, 2013, 73(20):6310-22
  • Biochem Pharmacol, 2012, 83(4):452-61
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM; also potent to Aurora A/B, Abl(T315I). Phase 2.
  • Cell Stem Cell, 2012, 11(2):179-94
  • Cancer Res, 2013, 73(20):6310-22
  • Cancer Lett, 2013, 341(2):224-30
S1249 JNJ-7706621 JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
  • Mol Cancer Ther, 2014, 13(3):662-74
S1529 Hesperadin Hesperadin potently inhibits Aurora B with IC50 of 250 nM. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
  • Nat Commun, 2011, 2:316
  • Curr Biol, 2011, 21(16):1356-65
  • J Cell Biol, 2012, 199(2):251-68
S1451 Aurora A Inhibitor I Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.
  • J Neurosci, 2012, 32(32):11050-66
  • Carcinogenesis, 2012, 33(2):285-93
  • Nephrol Dial Transplant, 2013, 28(11):2744-53
Cat.No. Product Name Information Product Citations Customer Reviews
S2158 KW-2449 KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.
S1154 SNS-314 Mesylate SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.
  • Cancer Res, 2013, 73(20):6310-22
  • Exp Cell Res, 2012, 318(4):336-49
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
  • Cancer Res, 2013, 73(20):6310-22
  • Vet Comp Oncol, 2013, 10.1111/vco.12046
S1454 PHA-680632 PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
  • Cancer Res, 2013, 73(10):3168-80
  • Cancer Res, 2013, 73(20):6310-22
  • Stem Cells, 2012, 30(9):1819-30
S2770 MK-5108 (VX-689) MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. Phase 1.
  • Cancer Discov, 2013, 10.1158/2159-8290.CD-12-0426
  • Oncogene, 2014, 33(27):3550-60
  • Cancer Lett, 2013, 341(2):248-64
S1171 CYC116 CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.
  • Cancer Res, 2013, 73(20):6310-22
S2719 AMG-900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2. Phase 1.
  • Br J Pharmacol, 2012, 166(3):858-76
S1519 CCT129202 CCT129202 is an ATP-competitive pan-Aurora inhibitor for Aurora A, Aurora B and Aurora C with IC50 of 0.042 μM, 0.198 μM and 0.227 μM, respectively. It is less potent to FGFR3, GSK3β, PDGFRβ, etc.
  • Cancer Res, 2013, 73(20):6310-22
  • Mol Pharm, 2012, 9(7):1971-82
S2725 PF-03814735 PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
  • Cancer Res, 2014, 10.1158/0008-5472.CAN-14-1009
S2740 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
  • Br J Pharmacol, 2012, 166(3):858-76
Cat.No. Product Name Information Product Citations Customer Reviews
S2718 TAK-901 TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
S2744 CCT137690 CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.
S2018 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
Tags: Aurora Kinase inhibition | Aurora Kinase cancer | Aurora A activation | Aurora A phosphorylation | Aurora B phosphorylation | Aurora B activation | Aurora Kinase assay | Aurora Kinase pathway | Aurora A and ic50 | Aurora Kinase inhibitors ic50 | Aurora Kinase inhibitor clinical trial | Aurora Kinase inhibitors as anticancer agents | Aurora Kinase inhibitor review
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