IG-105
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.
1: Li J, Si Y, Hu J, Liu L, Deng Y, He J, Zhang NM, Zhou D. Enhancing medical compliance of patients with convulsive epilepsy in rural community: a randomized intervention trial. Epilepsia. 2013 Nov;54(11):1988-96. doi: 10.1111/epi.12382. Epub 2013 Sep 30. PubMed PMID: 24117425.
2: Wang YM, Hu LX, Liu ZM, You XF, Zhang SH, Qu JR, Li ZR, Li Y, Kong WJ, He HW, Shao RG, Zhang LR, Peng ZG, Boykin DW, Jiang JD. N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide as a novel tubulin ligand against human cancer. Clin Cancer Res. 2008 Oct 1;14(19):6218-27. doi: 10.1158/1078-0432.CCR-08-0550. PubMed PMID: 18829501.
2: Wang YM, Hu LX, Liu ZM, You XF, Zhang SH, Qu JR, Li ZR, Li Y, Kong WJ, He HW, Shao RG, Zhang LR, Peng ZG, Boykin DW, Jiang JD. N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide as a novel tubulin ligand against human cancer. Clin Cancer Res. 2008 Oct 1;14(19):6218-27. doi: 10.1158/1078-0432.CCR-08-0550. PubMed PMID: 18829501.
| Chemical | |
|---|---|
| CAS Num | 905978-63-4 |
| Chemical Formula | C20H19N3O4S |
| Molecular Weight | 397.45 |
| IUPAC Chemical Name | N-(2,6-dimethoxypyridine-3-yl)-9-methylcarbazole-3-sulfonamide. |
| Exact Mass | 397.10963 |
| Elemental Analysis | C, 60.44; H, 4.82; N, 10.57; O, 16.10; S, 8.07 |
| Synonym | IG105; IG-105; IG 105. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=S(C1=CC2=C(C=C1)N(C)C3=C2C=CC=C3)(NC4=CC=C(OC)N=C4OC)=O |
| Biological | |
| Targets and Effects | microtubule inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | white solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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