Home>>Signaling Pathways>> Tyrosine Kinase>> EGFR>>MTX-531

MTX-531

目录号 : GC74012

MTX-531是一种口服药物,抑制EGFR(IC50为14.7nM)和PI3K(PI3Kα、PI3Kβ、PI3Kγ和PI3Kδ的IC50值分别为6.4、233、8.3和1.1nM),具有抗肿瘤作用。

MTX-531 Chemical Structure

Cas No.:2791417-66-6

规格 价格 库存 购买数量
5 mg
¥1,620.00
现货
10 mg
¥2,610.00
现货
25 mg
¥5,220.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

Description

MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate perglycemia induced by PI3K inhibitors.

MTX-531 (0-10000 nM, 2 h) shows a concentration-dependent inhibitory effect on EGFR, P13K, and mTOR in CAL-33 cells[1].MTX-531 is 3.4 μM with EC50 in 293H cells[1].MTX-531 (10 μM, 8-24 h) activates PPARγ in 3T3-L1 cells[1].

MTX-531 (100 mg/kg, orally, single dose) inhibits EGFR and PI3K-mTOR pathway signaling in a time-dependent manner in mice[1]. MTX-531 (25 mg/kg, orally, once daily for 134-145 days) suppresses tumor proliferation in mice[1]. MTX-531 (100 mg/kg, orally, single dose) shows excellent tolerance in mice and uniquely does not cause the perglycemia commonly seen with PI3K inhibitors[1]. MTX-531 (100 mg/kg, orally, single dose) inhibits EGFR and PI3K-mTOR signaling and tumor growth in the HNSCC PDX model[1]. MTX-531 enhances MEK inhibition in CRC[1]. MTX-531 (100 mg/kg, orally, 0-35 days) combined with KRAS-G12C inhibitors suppresses tumor growth in mice with KRAS-G12C mutant colorectal cancer or pancreatic tumors[1].

References:
[1]. Christopher E Whitehead, et al. A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. Nat Cancer. 2024 Jul 11.

化学性质

Cas No. 2791417-66-6 SDF
分子式 C22H20ClN5O2S 分子量 453.94
溶解度 DMSO : 100 mg/mL (220.29 mM; Need ultrasonic) 储存条件 -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.2029 mL 11.0147 mL 22.0293 mL
5 mM 0.4406 mL 2.2029 mL 4.4059 mL
10 mM 0.2203 mL 1.1015 mL 2.2029 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置

产品文档

Quality Control & SDS

View current batch: