CAS NO: | 56124-62-0 |
生物活性 | Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-inducedPKCactivation withIC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | Valrubicin (AD 32) is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively. Valrubicin inhibits the binding of [3H]PDBu to PKC. Therefore, Valrubicin competes with the tumor promoter for the PKC binding site and prevents the latter from both interacting with the phospholipid and binding to PKC[1]. Valrubicin shows cytotoxic activity against squamous cell carcinoma (SCC) cell line colony formation, with IC50s and IC90s of 8.24 ± 1.60 μM and 14.81 ± 2.82 μM for UMSCC5 cells, 15.90 ± 0.90 μM, 29.84 ± 0.84 μM for UMSCC5/CDDP? cells, and 10.50 ± 2.39 μM, 19.00 ± 3.91 μM for UMSCC10b cells, respectively. Moreover, Valrubicin in combination with radiation enhances the cytotoxicity[2]. | ||||||||||||||||
体内研究 (In Vivo) | Valrubicin (3, 6, or 9 mg) reduces tumor growth at week 3 by intratumoral jection in hamster. Valrubicin (6 mg) combined with minimally cytotoxic irradiation (150, 250, or 350 cGy) causes significant tumor shrinkage in hamster[2]. Valrubicin (0.1 μg/μL) significantly reduces the number of infiltrating neutrophils in biopsies challenged with TPA at 24 h and attenuates chronic inflammation in mice. Valrubicin also decreases the expression levels of inflammatory cytokines in the acute model[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 723.64 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C34H36F3NO13 | ||||||||||||||||
CAS 号 | 56124-62-0 | ||||||||||||||||
中文名称 | 戊柔比星 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 125 mg/mL(172.74 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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