IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein substrate. It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways.
CAS 905978-63-4 MFCD005978634
化学结构图
SMILES: COc1ccc(NS(=O)(=O)c2ccc3c(c2)c2ccccc2n3C)c(OC)n1
化学属性
| Mol. Weight | 397.45 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein substrate. It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways. |
|---|---|
| Formula | C20H19N3O4S |
| Synonym | IG105; IG-105; IG 105. |
| IUPAC Name | N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide. |
| InChIKey | JTPDYODKXJLRLA-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H19N3O4S/c1-23-17-7-5-4-6-14(17)15-12-13(8-10-18(15)23)28(24,25)22-16-9-11-19(26-2)21-20(16)27-3/h4-12,22H,1-3H3 |
| Canonical SMILES | O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O |
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- IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein substrate. It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways.
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