中文名 | 戊柔比星 |
英文名 | Valrubicin |
别名 | 缬柔比星 戊柔比星 戊柔吡星 戊柔比星(比星类) 戊柔比星(R&D) 戊柔比星 USP标准品 2-氧代-2-((2S,4S)-2,5,12-三羟基-4-(((2R,4S,5S,6S)-5-羟基-6-甲基-4-(2,2,2-三氟乙酰氨基)四氢-2H-吡喃-2-基)氧基)-7-甲氧基-6,11-二氧代-1,2,3,4,6,11-六氢并四苯-2-基)乙基 戊酸酯 |
英文别名 | ad32 nsc-246131 Valrubicin antibioticad32 trifluoroacetyl-adriamyci14-valerate trifluoroacetyladriamycin-14-valerate n-trifluoroacetyladriamycin14-valerate n-trifluoroacetyladriamycin-14-valerate n-trifluoroacetyldoxorubicin14-valerate [2-Oxo-2-[(2S,4S)-2,5,12-trihydroxy-4-[5-hydroxy-6-methyl-4-[(2,2,2-trifluoroacetyl)amino]oxan-2-yl]oxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]ethyl] pentanoate 2-oxo-2-[(2S,4S)-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-4-({2,3,6-trideoxy-3-[(trifluoroacetyl)amino]hexopyranosyl}oxy)-1,2,3,4,6,11-hexahydrotetracen-2-yl]ethyl pentanoate 2-oxo-2-[(2S,4S)-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-4-({2,3,6-trideoxy-3-[(trifluoroacetyl)amino]-alpha-L-lyxo-hexopyranosyl}oxy)-1,2,3,4,6,11-hexahydrotetracen-2-yl]ethyl pentanoate |
CAS | 56124-62-0 |
EINECS | 680-664-1 |
化学式 | C34H36F3NO13 |
分子量 | 723.64 |
InChI | InChI=1/C34H36F3NO13/c1-4-5-9-21(40)49-13-20(39)33(47)11-16-24(19(12-33)51-22-10-17(27(41)14(2)50-22)38-32(46)34(35,36)37)31(45)26-25(29(16)43)28(42)15-7-6-8-18(48-3)23(15)30(26)44/h6-8,14,17,19,22,27,41,43,45,47H,4-5,9-13H2,1-3H3,(H,38,46)/t14-,17-,19-,22-,27+,33-/m0/s1 |
密度 | 1.3473 (estimate) |
熔点 | 116-117 °C |
沸点 | 135-136 C |
闪点 | 478.6°C |
水溶性 | insoluble |
蒸汽压 | 3.81E-32mmHg at 25°C |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
折射率 | 1.618 |
酸度系数 | 7.34±0.60(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | Red |
体外研究 | Valrubicin (AD 32) is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC 50 s of 0.85 and 1.25 μM, respectively. Valrubicin inhibits the binding of [ 3 H]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. Valrubicin shows cytotoxic activity against squamous cell carcinoma (SCC) cell line colony formation, with IC 50 s and IC 90 s 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. |
体内研究 | 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. 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. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S37/39 - 戴适当的手套和护目镜或面具。 |
海关编号 | 2941906000 |
上游原料 | 吡啶 戊酸鈉 拓扑替康 阿霉素 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.382 ml | 6.91 ml | 13.819 ml |
5 mM | 0.276 ml | 1.382 ml | 2.764 ml |
10 mM | 0.138 ml | 0.691 ml | 1.382 ml |
5 mM | 0.028 ml | 0.138 ml | 0.276 ml |
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