228266-41-9
中文名称:228266-41-9
英文名称:Taltobulin (trifluoroacetate)
CAS号:228266-41-9
分子式:C29H44F3N3O6
分子量:587.6713696
EINECS号:
Mol文件:228266-41-9.mol
228266-41-9 用途与合成方法
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate) 是一种合成的三肽半胱氨酸类似物，Taltobulin 是一种有效的抗微管剂 (antimicrotubule)，可在体内外规避 P-糖蛋白介导的耐药性。Taltobulin trifluoroacetate 抑制纯化的微管蛋白聚合，破坏细胞中的微管组织，并诱导有丝分裂停滞以及凋亡 (apoptosis)。
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Traditional Cytotoxic Agents
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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. |
228266-41-9 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-02-08 | HY-15584A | 228266-41-9 | 228266-41-9 | 5mg | 2750 |
| 2025-02-08 | HY-15584A | 228266-41-9 | 228266-41-9 | 10mM * 1mLin DMSO | 3555 |
228266-41-9供应商 更多
上海一飞生物科技有限公司
联系电话：021-65675885 18964387627
产品介绍：
英文名称：Taltobulin (trifluoroacetate)
CAS：228266-41-9
纯度：95%
包装信息：2mg
备注：试剂级
北京普西唐生物科技有限公司
联系电话：010-60605840 18892239720
产品介绍：
英文名称：Taltobulin trifluoroacetate
CAS：228266-41-9
纯度：98%
包装信息：5mg
ChemeGen 中国
联系电话： 18818260767
产品介绍：
英文名称：Taltobulin trifluoroacetate
CAS：228266-41-9
纯度：98%
包装信息：10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
备注：品牌：ChemeGen
爱必信（上海）生物科技有限公司
联系电话：021-38015121 15000105423
产品介绍：
英文名称：Taltobulin trifluoroacetate
CAS：228266-41-9
纯度：98%
包装信息：5mg;10mg
天津普西唐生物医药科技有限公司
联系电话：010-60605840 15801484223;
产品介绍：
英文名称：Taltobulin trifluoroacetate
CAS：228266-41-9
纯度：98%
包装信息：5mg
