228266-41-9
| 中文名稱 | 228266-41-9 |
|---|---|
| 中文同義詞 | 化合物 T13073;化合物 TALTOBULIN TRIFLUOROACETATE |
| 英文名稱 | Taltobulin (trifluoroacetate) |
| 英文同義詞 | Taltobulin (trifluoroacetate);HTI-286 trifluoroacetate;HTI-286 TRIFLUOROACETATE;SPA-110 TRIFLUOROACETATE;SPA-110 trifluoroacetate |
| CAS號(hào) | 228266-41-9 |
| 分子式 | C29H44F3N3O6 |
| 分子量 | 587.6713696 |
| EINECS號(hào) | |
| 相關(guān)類別 | |
| Mol文件 | 228266-41-9.mol |
| 結(jié)構(gòu)式 |  |
228266-41-9 性質(zhì)
| 儲(chǔ)存條件 | Store at -20°C |
|---|---|
| 溶解度 | 二甲基亞砜：≥39mg/mL（66.36mM） |
| 形態(tài) | 固體 |
| 顏色 | 白色至米白色 |
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate) 是一種合成的三肽半胱氨酸類似物，Taltobulin 是一種有效的抗微管劑 (antimicrotubule)，可在體內(nèi)外規(guī)避 P-糖蛋白介導(dǎo)的耐藥性。Taltobulin trifluoroacetate 抑制純化的微管蛋白聚合，破壞細(xì)胞中的微管組織，并誘導(dǎo)有絲分裂停滯以及凋亡 (apoptosis)。
|
Traditional Cytotoxic Agents
|
Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC 50 of 2.5±2.1 nM and a median value of 1.7 nM.
Cell Proliferation Assay
| Cell Line: | Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines |
| Concentration: | 0.2-7.3 nM |
| Incubation Time: | 3 days |
| Result: | Inhibited the growth of tumor cell lines with IC 50 s of 0.2±0.03 nM (for leukemia CCRF-CEM cell line), 0.6±0.1 nM (for ovarian 1A9 cell line), 1.1±0.5 and 6.8±6.1 nM ( for NSCLC A549 and NCI-H1299 cell lines), 1.8±0.6, 7.3±2.3 nM (for breast MX-1W, MCF-7 cell lines), 0.7±0.2, 1.1±0.4, 1.5±0.6, 1.8±0.6, 3.6±0.8, 3.7±2.0, 4.2±2.5, and 5.3±4.1 nM ( for colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15, and Moser cell lines), 1.1±0.8, 1.4±0.6 and 1.7±0.5 nM (for melanoma A375, Lox and SK-Mel-2 cell lines). |
Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) in athymic nu/nu female mice.
Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively.
| Animal Model: | Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age) |
| Dosage: | 1.6 mg/kg |
| Administration: | Administered i.v.;for 35 days |
| Result: |
Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls.
Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls. Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls. Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively. |
安全信息
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-15584A | 228266-41-9 Taltobulin trifluoroacetate | 228266-41-9 | 5mg | 2750元 |
| 2024/11/08 | HY-15584A | 228266-41-9 Taltobulin trifluoroacetate | 228266-41-9 | 10mM * 1mLin DMSO | 3555元 |