| 中文名称: | 托西尼布 | ||||
|---|---|---|---|---|---|
| 英文名称: | Toceranib | ||||
| 别名: | SU11654; PHA 291639E | ||||
| CAS No: | 356068-94-5 | 分子式: | C22H25FN4O2 | 分子量: | 396.46 |
| CAS No: | 356068-94-5 | ||||
| 分子式: | C22H25FN4O2 | ||||
| 分子量: | 396.46 | ||||
熔点：
>133°C (dec.)
沸点：
596.8±50.0 °C(Predicted)
包装规格：
5mg 10mg 50mg in glass bottle
产品简介：
一种口服活性受体酪氨酸激酶 (RTK) 抑制剂，能有效抑制PDGFR，VEGFR，Kit，抑制 PDGFRβ 和 Flk-1/KDR 的 Ki 值分别为 5 nM 和 6 nM。Toceranib 具有抗肿瘤和抗血管生成活性，用于犬肥大细胞肿瘤的研究。
溶解性：
DMSO:2.5 mg/mL(6.31 mM;超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的DMSO)
Water：1 mg/mL (2.52 mM; 超声助溶 (<80°C))
Water：1 mg/mL (2.52 mM; 超声助溶 (<80°C))
储备液保存：
-80°C, 2 years
-20°C, 1 year
-20°C, 1 year
靶点：
PDGFRβ:5 nM (Ki)
Flk-1:6 nM (Ki)
体外研究：
Toceranib (SU11654) is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including PDGFR and Flk-1/KDR, with Kis of 5 and 6 nM, respectively.
To explore mechanisms of acquired Toceranib (TOC) resistance in canine MCT, three resistant sublines are generated from the Toceranib-sensitive exon 11 ITD c-kit mutant C2 cell line designated TR1, TR2, and TR3. Growth of the parental C2 cells is inhibited by Toceranib in a dose-dependent manner with an IC50 of <10 nM. In contrast, TR1, TR2, and TR3 sublines are resistant to inhibition by Toceranib (IC50> 1,000 nM). Sensitivity to three other KIT RTK inhibitors is similar to the observed resistance to Toceranib. The parental line as well as all three sublines retains sensitivity to the cytotoxic agents vinblastine (VBL) and CCNU. Following 72 hr culture in the presence of increasing concentrations of Toceranib, treatment naïve, parental C2 cells detach from the culture flask and become rounded, shrunken, and clumped with increased exposure to Toceranib. In contrast, Toceranib-induced morphologic differences are not identified in the resistant sublines.
To explore mechanisms of acquired Toceranib (TOC) resistance in canine MCT, three resistant sublines are generated from the Toceranib-sensitive exon 11 ITD c-kit mutant C2 cell line designated TR1, TR2, and TR3. Growth of the parental C2 cells is inhibited by Toceranib in a dose-dependent manner with an IC50 of <10 nM. In contrast, TR1, TR2, and TR3 sublines are resistant to inhibition by Toceranib (IC50> 1,000 nM). Sensitivity to three other KIT RTK inhibitors is similar to the observed resistance to Toceranib. The parental line as well as all three sublines retains sensitivity to the cytotoxic agents vinblastine (VBL) and CCNU. Following 72 hr culture in the presence of increasing concentrations of Toceranib, treatment naïve, parental C2 cells detach from the culture flask and become rounded, shrunken, and clumped with increased exposure to Toceranib. In contrast, Toceranib-induced morphologic differences are not identified in the resistant sublines.
体内研究：
Administration of Toceranib significantly decreases the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving Toceranib and cyclophosphamide (CYC) demonstrate a significant increase in serum concentrations of IFN-γ, which is inversely correlated with Treg numbers after 6 weeks of combination treatment.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
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参考文献 & 客户发表文献
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
