中文名 | 9-氨基喜树碱 |
英文名 | 9-Aminocamptothecin |
别名 | 9-氨基喜树碱 9-氨基喜树碱 标准品 (20S)-9-氨基喜树碱 9-氨基喜树碱,(20S)-9-氨基喜树碱 9-AMINOCAMPTOTHECIN 9-氨基喜树碱 |
英文别名 | AMinocaMptothecin 9-Aminocamptothecin 9-AMINO-CAMPTOTHECIN CAMPTOTHECIN, 9-AMINO- CAMPTOTHECIN, 9-AMINO-(RG) 9-Amino-20-(S)-camptothecin |
CAS | 91421-43-1 |
化学式 | C20H17N3O4 |
分子量 | 363.37 |
InChI | InChI=1/C20H17N3O4/c1-2-20(26)13-7-16-17-10(6-11-14(21)4-3-5-15(11)22-17)8-23(16)18(24)12(13)9-27-19(20)25/h3-7,26H,2,8-9,21H2,1H3/t20-/m0/s1 |
InChIKey | FUXVKZWTXQUGMW-FQEVSTJZSA-N |
密度 | 1.55±0.1 g/cm3(Predicted) |
熔点 | 142.0-145.0 °C |
沸点 | 819.6±65.0 °C(Predicted) |
闪点 | 449.5°C |
蒸汽压 | 2.01E-28mmHg at 25°C |
溶解度 | DMSO: 3.33毫克/毫升 (9.16毫米; 需要超声波) |
折射率 | 1.771 |
酸度系数 | 11.23±0.20(Predicted) |
存储条件 | 2-8°C(protect from light) |
外观 | 粉末或结晶 |
颜色 | Light yellow to Yellow to Orange |
Merck | 14,431 |
物化性质 | 黄色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于珙桐科植物喜树Camptotheca acuminata Decne.的果实。 |
MDL号 | MFCD00909855 |
体外研究 | In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC 50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure. |
体内研究 | 9-amino-CPT (9-amino-20(S)-camptothecin) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-amino-CPT (9-amino-20(S)-camptothecin) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-amino-CPT (9-amino-20(S)-camptothecin) induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML. |
RTECS | UQ0490500 |
海关编号 | 29349990 |