IRC-083927 is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two human tumor xenografts in nude mice (C33-A, human cervical cancer and MDA-MB-231, human hormone-independent breast cancer). Together, the antitumor effects induced by IRC-083927 on tumor models resistant to tubulin agents support further investigations to fully evaluate its potential for the treatment of advanced cancers, particularly those resistant to current clinically available drugs.
CAS 955082-09-4 MFCD055082094
化学结构图
SMILES: Cl.NS(=O)(=O)Nc1ccc(Oc2ccc(-c3cnc(COc4ccccc4)[nH]3)cc2)cc1F
化学属性
| Mol. Weight | 454.47 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | IRC-083927 is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two human tumor xenografts in nude mice (C33-A, human cervical cancer and MDA-MB-231, human hormone-independent breast cancer). Together, the antitumor effects induced by IRC-083927 on tumor models resistant to tubulin agents support further investigations to fully evaluate its potential for the treatment of advanced cancers, particularly those resistant to current clinically available drugs. |
|---|---|
| Formula | C22H19FN4O4S |
| Synonym | IRC083927; IRC 083927; IRC-083927. |
| IUPAC Name | Sulfamide, N-[2-fluoro-4-[4-[2-(phenoxymethyl)-1H-imidazol-5-yl]phenoxy]phenyl]-, hydrochloride. |
| InChIKey | WDKXZCKBBNZPLY-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H19FN4O4S.ClH/c23-19-12-18(10-11-20(19)27-32(24,28)29)31-17-8-6-15(7-9-17)21-13-25-22(26-21)14-30-16-4-2-1-3-5-16;/h1-13,27H,14H2,(H,25,26)(H2,24,28,29);1H |
| Canonical SMILES | O=S(N)(NC1=CC=C(OC2=CC=C(C3=CN=C(COC4=CC=CC=C4)N3)C=C2)C=C1F)=O.[H]Cl |
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- IRC-083927 is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two human tumor xenografts in nude mice (C33-A, human cervical cancer and MDA-MB-231, human hormone-independent breast cancer). Together, the antitumor effects induced by IRC-083927 on tumor models resistant to tubulin agents support further investigations to fully evaluate its potential for the treatment of advanced cancers, particularly those resistant to current clinically available drugs.
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