228266-41-9
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- CAS号:
- 228266-41-9
- 英文名:
- Taltobulin (trifluoroacetate)
- 英文别名:
- SPA-110 trifluoroacetate;HTI-286 trifluoroacetate;Taltobulin (trifluoroacetate);HTI-286 TRIFLUOROACETATE;SPA-110 TRIFLUOROACETATE
- 中文名:
- 228266-41-9
- 中文别名:
- 化合物 T13073
- CBNumber:
- CB42735540
- 分子式:
- C29H44F3N3O6
- 分子量:
- 587.6713696
- MOL File:
- 228266-41-9.mol
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228266-41-9化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 39 mg/mL (66.36 mM)
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228266-41-9性质、用途与生产工艺
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
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Cell Line:
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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
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Concentration:
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0.2-7.3 nM
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Incubation Time:
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3 days
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Result:
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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).
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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.
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Animal Model:
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Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)
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Dosage:
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1.6 mg/kg
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Administration:
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Administered i.v.;for 35 days
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Result:
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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.
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228266-41-9
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-15584A | 228266-41-9
Taltobulin trifluoroacetate | 228266-41-9 | 5mg | 2750元 |
| 2024/01/25 | HY-15584A | 228266-41-9
Taltobulin trifluoroacetate | 228266-41-9 | 10mM * 1mLin DMSO | 3555元 |
228266-41-9, 228266-41-9 相关搜索:
- 化合物 T13073
- 228266-41-9
- SPA-110 trifluoroacetate
- HTI-286 TRIFLUOROACETATE;SPA-110 TRIFLUOROACETATE
- HTI-286 trifluoroacetate
- Taltobulin (trifluoroacetate)