Cas No.: | 934541-31-8 |
Chemical Name: | TAK-901 |
Synonyms: | TAK901;TAK-901;5-(3-(Ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide;5-(3-ethylsulfonylphenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide;5-[3-(Ethylsulfonyl)phenyl]-3,8-dimethyl-N-(1-methyl-4-piperidinyl)-9H-pyrido[2,3-b]indole-7-carboxamide;PACLITAXEL C;5-[3-(Ethylsulfonyl)phenyl]-3,8-dimethyl-N-(1-methyl-4-piperidinyl)-9H-pyrido[2,3-b]indole-7-carboxamide (ACI);TAK 901;NCGC00346645-05;GLXC-03276;NSC803712;HY-12201;WKDACQVEJIVHMZ-UHFFFAOYSA-N;SB19309;CHEMBL3544932;DB12756;EX-A874;J-516603;HMS3656F17;SMR004701282;SW220051-1;MFCD18782651;NSC762151;AC-32836;NS00072151;SCHEMBL645679;NSC-762151;DB-044972;SDCCGSBI-0654430.P001;AS-19385;UNII-DM9UIR23R7;MLS006010174;AKOS005266666;5-[3-(ethanesulfonyl)phenyl]-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9H-pyrido[2,3-b]indole-7-carboxamide;NCGC00346645-01;CCG-269734;934541-31-8;Z2037281050;s2718;BRD-K01683783-001-02-6;9H-PYRIDO(2,3-B)INDOLE-7-CARBOXAMIDE, 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYL-4-PIPERIDINYL)-;DM9UIR23R7;Q27276478;DTXSID70583097;CS-0243;NCGC00346645-04;NSC-803712;NCGC00346645-03 |
SMILES: | O=C(C1C(C)=C2C(C3C(N2)=NC=C(C)C=3)=C(C2C=C(S(CC)(=O)=O)C=CC=2)C=1)NC1CCN(C)CC1 |
Formula: | C28H32N4O3S |
M.Wt: | 504.643685340881 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).It also inhibits JAK3, c-Src, CLK2, FGR, YES1, LRRK2, FLT3, Fyn, Abl, and FGFR2 (IC50s = 1.2-6.4 nM) and several other kinases. TAK-901 inhibits Aurora kinase complexes with IC50 values of 21 and 15 nM for the Aurora A and targeting protein for Xklp2 (TPX2) and Aurora B and inner centromere protein (INCENP) complexes, respectively. It decreases histone H3 phosphorylation in human prostate PC3 cancer cells (EC50 = 0.16 μM) and inhibits c-Src, FAK, FGFR2, FLT3, Abl, and Axl autophosphorylation in a panel of cancer cell lines (EC50s = 0.19-3.7 μM). TAK-901 inhibits the growth of lung, colon, stomach, skin, kidney, breast, ovarian, uterine, and prostate cancer cell lines (EC50s = 0.043-1.5 μM). In vivo, TAK-901 (40 mg/kg per day, i.v.) inhibits histone H3 phosphorylation and reduces tumor growth in an A2780 ovarian cancer nude rat xenograft model. TAK-901 also inhibits tumor growth in colorectal, acute myeloid leukemia (AML), and chronic myeloid leukemia (CML) mouse xenograft models. |