化学性质:
规格 | 10mM (in 1mL DMSO) 10mg 25mg 50mg |
CAS | 143-67-9 |
别名 | Vincaleukoblastine sulfate salt |
化学名 | N/A |
分子式 | C46H60N4O13S |
分子量 | 909.05 |
溶解度 | ≥ 28.85 mg/mL in DMSO, ≥ 48.2 mg/mL in H2O with ultrasonic |
储存条件 | 4°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
Description: IC50 Value: VIN showed EC50 values of 15 ug/ml, against P815 mastocytoma cells in-vitro[1]. Also supresses nAChR activity with IC50 of 8.9 μM. Vinblastine can inhibit the formation of microtubule, it also inhibit nAChR. It is a anticancer drug. More and more drug combination was investigated in clinical status. in vitro: At vinblastine concentrations of 0.5 uM and 2 uM, considerable inhibition of metabolic degradation of vinblastine was observed by competitive inhibitors of CYP3A4 (up to 60% inhibition), 2D6 (30%) and 2E1 (24%), while only a minor effect was observed for 2C9 (14%) and inhibitors of 1A2, 2C8 had no inhibitory effect on vinblastine metabolism. Vinblastine (0.5 and 2 uM) inhibited the metabolic capacity of CYP2C9 (up to 56%), 2C8 (36%), 2D6 (22%) and 3A4-mediated nifedipine oxidation (99%), while 3A4-mediated testosterone 6-beta-hydroxylation (max. 16%) as well as 1A2 and 2E1 remained unaffected[3]. in vivo: In combined intraperitoneal injection with vinblastine (200 micrograms kg-1) into P388/ADR-bearing mice, NA-382 in a suspension form (10 mg kg-1) prolonged the life-span of the mice near to that of P388/S-bearing mice treated with vinblastine alone, but verapamil even at the maximum tolerated dosage (30 mg kg-1) barely affected the in-vivo antitumour effect of vinblastine[2]. Clinical trial: Combination Chemotherapy With or Without Interleukin-2 and Interferon Alfa in Treating Patients With Metastatic Melanoma . Phase 3 Clinical
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