产品描述: | Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM. |
靶点: |
HSP90:0.71 nM (Kd);HSP |
体内研究: |
Onalespib (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts. Onalespib (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts |
参考文献: |
1. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53 2. Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.442 ml |
12.209 ml |
24.419 ml |
5 mM |
0.488 ml |
2.442 ml |
4.884 ml |
10 mM |
0.244 ml |
1.221 ml |
2.442 ml |
50 mM |
0.049 ml |
0.244 ml |
0.488 ml |
|
注意: |
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