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ChemicalBook CAS数据库列表 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

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 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-缬氨酰胺试剂级价格

CAS号:228266-40-8
英文名:TANDUTINIB
中文名: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
CBNumber:CB52131222
分子式:C27H43N3O4
分子量:473.66
MOL File:228266-40-8.mol

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-缬氨酰胺化学性质

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 :DMSO: 40 mg/ml
形态 :A solid
酸度系数(pKa) :4.68±0.19(Predicted)
颜色 :White to off-white

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、用途与生产工艺

生物活性 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)。
靶点

Traditional Cytotoxic Agents

体外研究

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).

体内研究

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.