CRT0273750
目录号: PL06768 纯度: ≥98%
CAS No. :1979939-16-6
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中文名称
CRT0273750
英文名称
CRT0273750
英文别名
CRT0273750;(S)-N-(1-(4-Chlorophenyl)ethyl)-3-(3-(4-(trifluoromethoxy)benzyl)-3H-imidazo[4,5-b]pyridin-2-yl)propanamide;BDBM50200622;ClC1=CC=C(C=C1)[C@H](C)NC(CCC1=NC=2C(=NC=CC=2)N1CC1=CC=C(C=C1)OC(F)(F)F)=O;6XN
Cas No.
1979939-16-6
分子式
C25H22ClF3N4O2
分子量
502.92
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
CRT0273750 是 ATX 抑制剂的先导化合物,并调节血浆中 LPA 水平。CRT0273750 可用于 ATX/LPA 依赖性癌症模型。
生物活性
CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC 50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer.
性状
Solid
IC50 & Target[1][2]
IC50: 0.014 μM (plasma CRA)
体外研究(In Vitro)
CRT0273750 shows high potency in both the biochemical (IC50 = 0.01 μM) and plasma choline release assay(IC50 = 0.014 μM).
CRT0273750 is also shown to inhibit the migration of 4T1 cells with an EC50 of 0.025μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
CRT0273750 (1 mg/kg; i.v.)has a moderate blood clearance, with value of 41 mL/min/kg.
CRT0273750 (10 mg/kg; oral administration) treatment shows the C max , AUC and t 1/2 values of 3.8 μM, 3.2 μM.h and 1.4 h, respectively.
CRT0273750 (10, 30 and 100 mg/kg; oral administration) shows a proportional increase. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Shah P, et al. Discovery of potent inhibitors of the lysophospholipase autotaxin. Bioorg Med Chem Lett. 2016;26(22):5403-5410.
溶解度数据
In Vitro: DMSO : 250 mg/mL (497.10 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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