Talabostat mesylate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值:1 nM
Talabostat mesilate(PT-100, Val-boroPro)是一种具有口服活性的DPP4二肽基肽酶特异性抑制剂,包括肿瘤相关的成纤维细胞活化蛋白-(FAP).
成纤维细胞活化蛋白-(FAP)是一种整合膜丝氨酸蛋白酶,也是后脯氨酰肽酶家族的成员,与二肽基肽酶IV(DPPIV)密切相关,并具有/-水解酶和八股-螺旋桨域的特点,呈现DPPIV样折叠[1].
体外:通过剪切N端Xaa-Pro或Xaa-Ala残基,talabostat可阻断二肽基肽酶,如成纤维细胞活化蛋白(FAP),从而诱导细胞因子和趋化因子(除了特异性的T细胞免疫和T细胞依赖的活性)的产生.该物质也可诱导集落刺激因子的产生,如粒细胞集落刺激因子(G-CSF),从而诱导造血.二肽基肽酶与多肽激素和趋化因子激活有关.
Talabostat可轻微降低表达FAP的肿瘤的生长速率,但由于PT-630和LAF-237不能,这一生长阻断可能与抑制FAP或相关的后脯氨酰肽酶二肽基肽酶IV无关.[1]
体内:迄今为止,无体内实验进行.
临床试验:临床研究未进行.
参考文献:
[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.
- 1. Andreas Linder, Stefan Bauernfried, et al. "CARD8 inflammasome activation triggers pyroptosis in human T cells." EMBO J 2020 Aug 25;e105071. PMID:32840892
- 2. 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
- 3. 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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 310.18 |
Cas No. | 150080-09-4 |
Formula | C10H23BN2O6S |
Solubility | ≥11.45 mg/mL in DMSO; ≥31 mg/mL in H2O; ≥8.2 mg/mL in EtOH with ultrasonic |
SDF | Download SDF |
Canonical SMILES | OS(=O)(C)=O.O=C([C@H](C(C)C)N)N1[C@H](B(O)O)CCC1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
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. |
质量控制和MSDS
- 批次: