MTX-531
目录号 : GC74012MTX-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。
Cas No.:2791417-66-6
Sample solution is provided at 25 µL, 10mM.
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.
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。 |
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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。 |
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 |
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 | 只 | |||
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 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
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