905978-63-4
Chemical Structure
IG-105
- CAS No.: 905978-63-4
- Formula:C20H19N3O4S
- Molecular Weight:397.45
IUPAC Name: N-(2,6-dimethoxypyridin-3-yl)-9-methyl-9H-carbazole-3-sulfonamide
InChIKey: JTPDYODKXJLRLA-UHFFFAOYSA-N
SMILES: O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O
Biological Activity: IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [3H] colchicine binding to tubulin with an IC50 of 0.6 μM and inhibits tubulin polymerization with an IC50 of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer[1][2].
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IG-105 | IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [3H] colchicine binding to tubulin with an IC50 of 0.6 μM and inhibits tubulin polymerization with an IC50 of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer. | |||||||||||||||||||||
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References
- [1]. Wang YM, et al. N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide as a novel tubulin ligand against human cancer. Clinical cancer research : an official journal of the American Association for Cancer Research. 2008 Oct 01;14(19):6218-27. [Content Brief]
- [2]. Pang J, et al. Simplified LC-MS/MS method for quantification of IG-105, a novel tubulin ligand, and its application to the pharmacokinetic study in rats at the anticancer effective dose. Pharmazie. 2019 Feb 1;74(2):79-82.
