N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺
生物活性靶点体外研究体内研究 用途与合成方法 MSDS N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺价格(试剂级) 上下游产品信息
| 中文名称 | N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺 |
|---|---|
| 中文同义词 | N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺;他托布林;化合物TALTOBULIN;(S,E)-2,5-二甲基-4-((S)-N,3,3-三甲基-2-((S)-3-甲基-2-(甲氨基)-3-苯基丁酰胺基)丁酰胺基)己-2-烯酸 |
| 英文名称 | TANDUTINIB |
| 英文同义词 | N,beta,beta-Trimethyl-L-phenylalanyl-N-[(1S,2E)-3-carboxy-1-(1-methylethyl)-2-butenyl]-N,3-dimethyl-L-valinamide;Hti 286;L-Valinamide, N,beta,beta-trimethyl-L-phenylalanyl-N-((1S,2E)-3-carboxy-1-(1-methylethyl)-2-butenyl)-N,3-dimethyl-;Spa 110;Unii-J6D6912bxs;Taltobulin;N,β,β-Trimethyl-L-phenylalanyl-N-[(3S,4E)-5-carboxy-2-methyl-4-hexen-3-yl]-N,3-dimethyl-L-valinamide;CS-1371 |
| CAS号 | 228266-40-8 |
| 分子式 | C27H43N3O4 |
| 分子量 | 473.66 |
| EINECS号 | |
| 相关类别 | 医药原料药;日用化学品;标准品 |
| Mol文件 | 228266-40-8.mol |
| 结构式 | ![N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺 结构式](CAS/GIF/228266-40-8.gif) |
N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺 性质
| 熔点 | 135-137 ºC |
|---|---|
| 沸点 | 662.4±55.0 °C(Predicted) |
| 密度 | 1.063 |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 二甲基亚砜：40mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.68±0.19(Predicted) |
Taltobulin (HTI-286) 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 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)。
|
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 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-15584 | Taltobulin | 1 mg | 1045元 | |
| 2024/01/25 | HY-15584 | N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺 Taltobulin | 228266-40-8 | 5mg | 2300元 |