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Talabostat mesylate

现货
Catalog No.
B3941
DPP4抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,960.00
现货
10mg
¥ 1,780.00
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50mg
¥ 7,500.00
现货

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Background

IC50: 1 nM

Talabostat mesilate (PT-100; Val-boroPro) is an orally active, specific inhibitor of dipeptidyl peptidases for DPP4, including tumor-associated fibroblast activation protein- (FAP).

Fibroblast activation protein- (FAP), as an integral membrane serine protease and member of the post-prolyl peptidase family, closely related to dipeptidyl peptidase IV (DPPIV) and displays a DPPIV-like fold with the characteristic /-hydrolase and eightbladed -propeller domains [1].

In vitro: By the cleavage of N-terminal Xaa-Pro or Xaa-Ala residues, talabostat blocks dipeptidyl peptidases, such as fibroblast activation protein (FAP), resulting in inducing the production of cytokine and chemokine (besides specific T-cell immunity and T-cell-dependent activity). This agent may also induce the production of colony stimulating factors, for instance, granulocyte colony stimulating factor (G-CSF), resulting in the inducement of hematopoiesis. Dipeptidyl peptidases are referred to the activation of polypeptide hormones and chemokines.

Talabostat slightly lowered the growth rates of the FAP-expressing tumors but because PT-630 and LAF-237 did not, the growth blockade was likely not related to inhibit FAP or the related post-prolyl peptidase dipeptidyl peptidase IV.[1]

In vivo: So far, no study in vivo has been conducted.

Clinical trial: Clinical study has been conducted.

Reference:
[1].  Huang Y, Simms AE, Mazur A, Wang S, León NR, Jones B, Aziz N, Kelly T. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79.

文献引用

1. Chen M, Lei X, et al. "Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents." J Clin Invest. 2017 Oct 2;127(10):3689-3701. PMID:28846068
2. Feng X, Wang Q, et al. "A synthetic urinary probe-coated nanoparticles sensitive to fibroblast activation protein α for solid tumor diagnosis." Int J Nanomedicine. 2017 Jul 27;12:5359-5372. PMID:28794628

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt310.18
Cas No.150080-09-4
FormulaC10H23BN2O6S
Solubility≥11.45mg/mL in DMSO
SDFDownload SDF
Canonical SMILESOS(=O)(C)=O.O=C([C@H](C(C)C)N)N1[C@H](B(O)O)CCC1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

MDA MB-435细胞和人类乳腺癌细胞系WTY-1和WTY-6

制备方法

该化合物可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

10 μM

实验结果

在不表达FAP的MDA MB-231细胞中,Talabostat在FAP活性测定中没有显示出任何作用。在表达野生型和活性FAP的WTY-1和WTY-6细胞中,Talabostat显著抑制其FAP活性。

动物实验 [1]:

动物模型

携带人类乳腺癌细胞系WTY-1和WTY-6以及MDA MB-435细胞的SCID小鼠

给药剂量

1.3 mg/kg;口服给药;每天1次

实验结果

在携带人类乳腺癌细胞系WTY-1和WTY-6以及MDA MB-435细胞的SCID小鼠中,Talabostat稍微减缓肿瘤生长。在携带MDA MB-435细胞的小鼠中,Talabostat延迟肿瘤形成(约12天),然而,上述作用无统计学差异。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Huang Y, Simms AE, Mazur A, Wang S, León NR, Jones B, Aziz N, Kelly T. Fibroblast activation protein-α promotes tumor growth and invasion of breast cancer cells through non-enzymatic functions. Clin Exp Metastasis. 2011 Aug;28(6):567-79.

质量控制

化学结构

Talabostat mesylate

相关生物数据

Talabostat mesylate

相关生物数据

Talabostat mesylate