IRC-083927
IRC-083927 is an orally active tubulin inhibitor. IRC-083927 binds competitively to the colchicine-binding site on tubulin, inhibits tubulin polymerization, disrupts the microtubule cytoskeleton, and arrests the cell cycle at the G2-M phase. IRC-083927 can be used in research related to human cervical cancer, hormone-independent breast cancer, pancreatic cancer, prostate cancer, and small cell lung cancer.
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- No. CAS: 955157-23-0
- Fòrmula: C22H19FN4O4S
- Peso molecular:454.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
IRC-083927 (5-100 nM) hydrochloride disrupts and depolymerizes the microtubule cytoskeleton in human prostate cancer DU-145 cells[1].
IRC-083927 (72-96 h) hydrochloride inhibits the proliferation of human tumor cell lines including MIA PaCa-2, MDA-MB-231, DU-145, NCI-H69, NCI-H69/AR, NCI-H69/Lx4, A549, A549.EpoB40 and A549.EpoB480, with IC50 values ranging from 7 μM to 42 μM. It remains active against cell lines that develop resistance to standard tubulin-binding agents via efflux pumps or tubulin mutations[1].
IRC-083927 (10-20 nM; 11 days) hydrochloride inhibits endothelial cell proliferation and blocks angiogenesis in human umbilical vein endothelial cells (HUVECs) and their co-culture system with fibroblasts[1].
IRC-083927 (10-60 nM; 24 h) hydrochloride arrests the cell cycle at the G2-M phase in human non-small cell lung cancer A549 cell line and its tubulin mutation-resistant A549.EpoB40 cells[1].
IRC-083927 (5 μM; 60 min) hydrochloride inhibits tubulin polymerization in purified bovine brain tubulin[1].
IRC-083927 (20 μM; 3 h) hydrochloride competitively inhibits the binding of labeled colchicine to purified tubulin in a cell-free system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 and A549.EpoB40 cell lines
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Concentration:10, 30, 60 nM
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Incubation Time:24 h
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Result:Decreased the percentage of cells in the G0-G1 phase and caused a massive accumulation and arrest of cells in the G2-M phase in a concentration-dependent manner.
In Vivo
IRC-083927 (5 mg/kg; administered orally; once daily for 5 consecutive days followed by 2 days of withdrawal; treated continuously for 4 weeks) hydrochloride exerts a significant tumor growth inhibitory effect in a mouse model of subcutaneous xenografted human breast cancer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic NCr-nu/nu (female, 4- to 6-week-old, human cervical C33-A tumor cells s.c. injected into flanks)[1]
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Dosage:2.5 mg/kg; 5 mg/kg
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Administration:p.o.; once daily for 5 days, 2 days off, repeated for 4 weeks
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Result:Significantly inhibited tumor growth and reduced tumor volume with a certain degree of dose relevance at both the end of the treatment period and the end of the follow-up period.
Caused no apparent macroscopic toxicity throughout the treatment; animals did not experience weight loss or death.
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Animal Model:athymic NCr-nu/nu (female, 4- to 6-week-old, human hormone-independent MDA-MB-231 breast tumor cells s.c. injected into flanks)[1]
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Dosage:5 mg/kg
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Administration:p.o.; once daily for 5 days, 2 days off, repeated for 4 weeks
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Result:Significantly inhibited breast tumor growth, leading to stabilization of the tumor volume during the treatment period.
Induced no significant body weight loss or related adverse toxicities in the mice.
Chemical Information
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No. CAS 955157-23-0
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Peso molecular 454.47
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Fòrmula C22H19FN4O4S
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SMILES
O=S(N)(NC1=CC=C(C=C1F)OC2=CC=C(C3=CN=C(COC4=CC=CC=C4)N3)C=C2)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Liberatore AM, et al. IRC-083927 is a new tubulin binder that inhibits growth of human tumor cells resistant to standard tubulin-binding agents. Molecular cancer therapeutics. 2008 Aug;7(8):2426-34. [Content Brief]
[2]. Chen SM, et al. New microtubule-inhibiting anticancer agents. Expert opinion on investigational drugs. 2010 Mar;19(3):329-43. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IRC-083927 Related Classifications
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