Anticancer agent 98
Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min.
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: 2857070-72-3
- 分子式: C17H19N5O2
- 分子量:325.37
-
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
Anticancer agent 98 inhibits cancer proliferation among melanoma, breast cancer, and pancreatic cancer with IC50s ranging from 0.6-3 nM[1].
Anticancer agent 98 (300 nM, 1 μM, or 3 μM; 2 h) increases β-tubulin adduct in PC-3 cells dose-dependently[1].
Anticancer agent 98 (3.125, 6.25, 12.5, 25, and 50 μM) has high-binding affinity to tubulin proteins with Kd value of 16.9 μM by SPR spectroscopy assay[1].
Anticancer agent 98 (10 μM, 50 μM; 0-60 min) strongly inhibits tubulin polymerization during 60 min[1].
Anticancer agent 98 (100 nM; 4 h) has antiproliferative and anti-angiogenesis effect on COS-7 cells in vitro[1].
In Vitro Metabolic Stability[1]
| human microsomes | mouse microsomes | ||
| t1/2 (min) | CLint (μL/min/mg) | t1/2 (min) | CLint (μL/min/mg) |
| >300 | <2.31 | >300 | <2.31 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Analysis in NSG Mice[1]
| Route | Dose (mg/kg) | Cmax (ng/mL) | tmax (min) | AUC (ng·min/mL) | t1/2 (min) | F (%) |
| i.v. | 4 | 1247 | 5.0 | 173,476 | 238 | / |
| p.o. | 10 | 78.3 | 10.0 | 8161 | 358 | 2.02 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:PC3/TxR xenograft model in NSG mouse[1]
-
Dosage:2.5 mg/kg
-
Administration:IV; twice weekly for 2 weeks
-
Result:Inhibited the tumor growth in volume by approximately 85.6%. And inhibited angiogenesis by 44% related to control group.
Overcame taxane resistance at a low, safe, but potent dose in vivo.
化学情報
-
CAS 番号 2857070-72-3
-
分子量 325.37
-
分子式 C17H19N5O2
-
SMILES
O=C1NC2=CC(OC)=CC=C2N(C1)C3=NC(NC)=NC4=C3CCC4
-
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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Anticancer agent 98 関連分類
HY-149920 関連分類
Powered by Bioz