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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 955157-23-0
- 分子式: C22H19FN4O4S
- 分子量:454.47
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
体外実験
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.
-
Cell Line:A549 and A549.EpoB40 cell lines
-
Concentration:10, 30, 60 nM
-
Incubation Time:24 h
-
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.
体内実験
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.
-
Animal Model:athymic NCr-nu/nu (female, 4- to 6-week-old, human cervical C33-A tumor cells s.c. injected into flanks)[1]
-
Dosage:2.5 mg/kg; 5 mg/kg
-
Administration:p.o.; once daily for 5 days, 2 days off, repeated for 4 weeks
-
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.
-
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]
-
Dosage:5 mg/kg
-
Administration:p.o.; once daily for 5 days, 2 days off, repeated for 4 weeks
-
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.
化学情報
-
CAS 番号 955157-23-0
-
分子量 454.47
-
分子式 C22H19FN4O4S
-
SMILES
O=S(N)(NC1=CC=C(C=C1F)OC2=CC=C(C3=CN=C(COC4=CC=CC=C4)N3)C=C2)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
IRC-083927 関連分類
HY-111015A 関連分類
Powered by Bioz