Aurora Kinase

シグナル伝達経路

Aurora Kinaseシグナル伝達経路

Aurora Kinase製品

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  • Aurora Kinase阻害剤 (38)
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S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Sci Rep, 2024, 14(1):4303
bioRxiv, 2024, 2024.01.17.575938
S1147 Barasertib (AZD1152-HQPA) Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):1041
Br J Cancer, 2024, 10.1038/s41416-024-02584-z
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Neoplasia, 2024, 48:100966
Nat Commun, 2023, 14(1):6505
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.
Nat Commun, 2024, 15(1):1041
Adv Sci (Weinh), 2023, 10(12):e2204388
EMBO J, 2023, e113510.
S1100 MLN8054 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
Nat Commun, 2024, 15(1):1041
Nat Commun, 2023, 14(1):5317
Mol Biol Cell, 2023, 34(5):ar47
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 in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
S1529 Hesperadin Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
Oncogene, 2022, 10.1038/s41388-022-02328-4
Cancers (Basel), 2022, 14(15)3732
Hum Cell, 2022, 10.1007/s13577-022-00675-8
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay 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. MK-5108 (VX-689) induces autophagy. Phase 1.
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
Sci Rep, 2022, 12(1):6345
S1451 TCS7010 (Aurora A Inhibitor I) TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
Int J Mol Sci, 2022, 23(24)15573
Biochim Biophys Acta Mol Cell Res, 2022, 1869(12):119361
Environ Mol Mutagen, 2022, 63(3):151-161
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I).
PeerJ, 2023, 11:e16581
bioRxiv, 2023, 10.1101/2023.12.19.572304
Cancers (Basel), 2022, 14(21)5215
S1249 JNJ-7706621 JNJ-7706621 is a 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 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Microbiol Spectr, 2023, 11(1):e0194322
Cancer Cell, 2022, S1535-6108(22)00312-9
Curr Biol, 2022, 32(19):4314-4324.e7
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Cancer Cell, 2022, 40(7):754-767.e6
Int J Mol Sci, 2022, 23(24)15573
S1454 PHA-680632 PHA-680632 is a 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.
Heliyon, 2023, 9(7):e17386
Signal Transduct Target Ther, 2022, 7(1):97
Front Cell Dev Biol, 2020, 8:590449
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Cancer Res, 2022, 82(11):2141-2155
S7588 Reversine Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2023, 14(1):3364
Commun Biol, 2023, 6(1):1271
Heliyon, 2023, 9(9):e20182
S1154 SNS-314 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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Res Sq, 2023, rs.3.rs-2570204
Haematologica, 2022, 10.3324/haematol.2022.280884
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 RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
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.
PLoS One, 2024, 19(1):e0295629
Cell Chem Biol, 2023, 30(8):987-998.e24
Cancer Cell, 2021, S1535-6108(21)00383-4
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Ecotoxicol Environ Saf, 2023, 265:115513
bioRxiv, 2023, 10.1101/2023.12.19.572304
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.
Sci Rep, 2024, 14(1):4303
Cell Chem Biol, 2023, 30(8):987-998.e24
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Microbiol Spectr, 2023, 11(1):e0194322
bioRxiv, 2023, 10.1101/2023.12.19.572304
S7843 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Nat Commun, 2023, 14(1):478
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
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.
Aging (Albany NY), 2020, 7;12(9):8221-8240
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
PLoS One, 2014, 9(7):e102741
S8699 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Haematologica, 2022, 10.3324/haematol.2022.280884
Cancers (Basel), 2021, 13(6)1205
Front Pharmacol, 2020, 30;11:543
S8782 LY3295668 LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
EBioMedicine, 2023, 95:104752
Cell Rep, 2022, 41(12):111826
Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469
S9658 SP-96 SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).
Cell Chem Biol, 2023, 30(8):987-998.e24
S7065 MK-8745 MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.
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.
S9741New TAS-119 TAS-119 is a potent, selective, and orally active inhibitor of Aurora A, including Aurora B with an IC50 of 1.0 nM and 95 nM, respectively. It exhibits antitumor activities.
E0338 AKI603 AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
E0342 Aurora kinase Inhibitor II Aurora kinase inhibitor II, an anilinoquinazoline that is both a potent and selective ATP-competitive inhibitor of Aurora kinase (ARK), has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division.
E0616 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
E1651New CD532 CD532 is a potent  Aurora A kinase inhibitor with an IC50 of 45 nM. It breaks the native conformation of Aurora-A, drives the degradation of N-Myc in N-Myc-driven cancers, and also exhibits anti-proliferative effects.
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
S1460 SP600125 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Nat Commun, 2024, 15(1):987
Acta Biomater, 2024, S1742-7061(24)00036-9
Cell Death Dis, 2024, 15(1):31
S1133 Alisertib (MLN8237) Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):1041
Sci Rep, 2024, 14(1):4303
bioRxiv, 2024, 2024.01.17.575938
S1147 Barasertib (AZD1152-HQPA) Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Gastroenterology, 2024, S0016-5085(24)00062-3
Nat Commun, 2024, 15(1):1041
Br J Cancer, 2024, 10.1038/s41416-024-02584-z
S1048 Tozasertib (VX-680) Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.
Cell Death Dis, 2024, 15(1):56
Neoplasia, 2024, 48:100966
Nat Commun, 2023, 14(1):6505
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.
Nat Commun, 2024, 15(1):1041
Adv Sci (Weinh), 2023, 10(12):e2204388
EMBO J, 2023, e113510.
S1100 MLN8054 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
Nat Commun, 2024, 15(1):1041
Nat Commun, 2023, 14(1):5317
Mol Biol Cell, 2023, 34(5):ar47
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 in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
Sci Rep, 2024, 14(1):4303
Proc Natl Acad Sci U S A, 2023, 120(34):e2304611120
Cell Chem Biol, 2023, 30(8):987-998.e24
S1529 Hesperadin Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
Oncogene, 2022, 10.1038/s41388-022-02328-4
Cancers (Basel), 2022, 14(15)3732
Hum Cell, 2022, 10.1007/s13577-022-00675-8
S2770 MK-5108 MK-5108 is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay 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. MK-5108 (VX-689) induces autophagy. Phase 1.
Sci Rep, 2024, 14(1):4303
Biosensors (Basel), 2022, 12(4)196
Sci Rep, 2022, 12(1):6345
S1451 TCS7010 (Aurora A Inhibitor I) TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.
Int J Mol Sci, 2022, 23(24)15573
Biochim Biophys Acta Mol Cell Res, 2022, 1869(12):119361
Environ Mol Mutagen, 2022, 63(3):151-161
S1134 AT9283 AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I).
PeerJ, 2023, 11:e16581
bioRxiv, 2023, 10.1101/2023.12.19.572304
Cancers (Basel), 2022, 14(21)5215
S1249 JNJ-7706621 JNJ-7706621 is a 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 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Microbiol Spectr, 2023, 11(1):e0194322
Cancer Cell, 2022, S1535-6108(22)00312-9
Curr Biol, 2022, 32(19):4314-4324.e7
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Cancer Cell, 2022, 40(7):754-767.e6
Int J Mol Sci, 2022, 23(24)15573
S1454 PHA-680632 PHA-680632 is a 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.
Heliyon, 2023, 9(7):e17386
Signal Transduct Target Ther, 2022, 7(1):97
Front Cell Dev Biol, 2020, 8:590449
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.
Cancer Cell, 2022, S1535-6108(22)00312-9
Cell Rep Med, 2022, 3(1):100492
Cancer Res, 2022, 82(11):2141-2155
S7588 Reversine Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 400 nM/500 nM/400 nM, respectively. Also used for stem cell dedifferentiation.
Nat Commun, 2023, 14(1):3364
Commun Biol, 2023, 6(1):1271
Heliyon, 2023, 9(9):e20182
S1154 SNS-314 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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Res Sq, 2023, rs.3.rs-2570204
Haematologica, 2022, 10.3324/haematol.2022.280884
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 RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
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.
PLoS One, 2024, 19(1):e0295629
Cell Chem Biol, 2023, 30(8):987-998.e24
Cancer Cell, 2021, S1535-6108(21)00383-4
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Ecotoxicol Environ Saf, 2023, 265:115513
bioRxiv, 2023, 10.1101/2023.12.19.572304
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.
Sci Rep, 2024, 14(1):4303
Cell Chem Biol, 2023, 30(8):987-998.e24
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
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.
Cell Chem Biol, 2023, 30(8):987-998.e24
Microbiol Spectr, 2023, 11(1):e0194322
bioRxiv, 2023, 10.1101/2023.12.19.572304
S7843 BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Nat Commun, 2023, 14(1):478
Cancer Res Commun, 2023, 3(10):2170-2181
Cancer Res Commun, 2023, 3(10):2170-2181
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.
Aging (Albany NY), 2020, 7;12(9):8221-8240
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
PLoS One, 2014, 9(7):e102741
S8699 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
Haematologica, 2022, 10.3324/haematol.2022.280884
Cancers (Basel), 2021, 13(6)1205
Front Pharmacol, 2020, 30;11:543
S8782 LY3295668 LY3295668 (AK-01) is a potent, orally active and specific inhibitor of Aurora A kinase with Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.
EBioMedicine, 2023, 95:104752
Cell Rep, 2022, 41(12):111826
Kaohsiung J Med Sci, 2021, 10.1002/kjm2.12469
S9658 SP-96 SP-96 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-96 can be used for the research of triple negative breast cancer (TNBC).
Cell Chem Biol, 2023, 30(8):987-998.e24
S7065 MK-8745 MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6 nM, more than 450-fold selectivity for Aurora A over Aurora B.
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.
S9741New TAS-119 TAS-119 is a potent, selective, and orally active inhibitor of Aurora A, including Aurora B with an IC50 of 1.0 nM and 95 nM, respectively. It exhibits antitumor activities.
E0338 AKI603 AKI-603 is an inhibitor of Aurora kinase A (AurA), which is developed to overcome resistance mediated by BCR-ABL-T315I mutation.
E0342 Aurora kinase Inhibitor II Aurora kinase inhibitor II, an anilinoquinazoline that is both a potent and selective ATP-competitive inhibitor of Aurora kinase (ARK), has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division.
E0616 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
S2931 Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent inhibitor of Aurora A kinase with an IC50 of 42 nM and has high selectivity for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively).
S6214 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
E1651New CD532 CD532 is a potent  Aurora A kinase inhibitor with an IC50 of 45 nM. It breaks the native conformation of Aurora-A, drives the degradation of N-Myc in N-Myc-driven cancers, and also exhibits anti-proliferative effects.
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).
S9741New TAS-119 TAS-119 is a potent, selective, and orally active inhibitor of Aurora A, including Aurora B with an IC50 of 1.0 nM and 95 nM, respectively. It exhibits antitumor activities.
E1651New CD532 CD532 is a potent  Aurora A kinase inhibitor with an IC50 of 45 nM. It breaks the native conformation of Aurora-A, drives the degradation of N-Myc in N-Myc-driven cancers, and also exhibits anti-proliferative effects.
E1435New Tinengotinib Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC).

Aurora Kinase阻害剤の選択性比較

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