228266-40-8
中文名稱
N,BETA,BETA-三甲基-L-苯基丙氨?；?N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-纈氨酰胺
英文名稱
TANDUTINIB
CAS
228266-40-8
分子式
C27H43N3O4
分子量
473.66
MOL 文件
228266-40-8.mol
更新日期
2024/11/15 18:20:33
228266-40-8 結(jié)構(gòu)式
基本信息
中文別名
N,BETA,BETA-三甲基-L-苯基丙氨?；?N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-纈氨酰胺 英文別名
CS-1371Spa 110
Hti 286
Taltobulin
Unii-J6D6912bxs
HTI-286
SPA-110
Taltobulin (HTI-286)
HTI-286 hydrochloride
SPA-110 hydrochloride
HTI-286 HYDROCHLORIDE
SPA-110 HYDROCHLORIDE
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)135-137 ºC
沸點(diǎn)662.4±55.0 °C(Predicted)
密度1.063
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度DMSO: 40 mg/ml
酸度系數(shù)(pKa)4.68±0.19(Predicted)
形態(tài)固體
顏色White to off-white
常見問題列表
生物活性
Taltobulin (HTI-286) 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 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)。靶點(diǎn)
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Traditional Cytotoxic Agents
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體外研究
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). |
體內(nèi)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. |