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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-MTX-531
MTX-531

Chemical Structure : MTX-531

CAS No.: 2791417-66-6

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MTX-531 (MTX531)

货号: PC-22758Not For Human Use, Lab Use Only.

MTX-531 (MTX531) is a first-in-class, potent and selective inhibitor of EGFR and PI3K with IC50 of 15  nM and 6.4  nM (PI3Kα), respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MTX-531 (MTX531) is a first-in-class, potent and selective inhibitor of EGFR and PI3K with IC50 of 15  nM and 6.4  nM (PI3Kα), respectively.
MTX-531 is exquisitely selective for HER (human EGFR) and PI3K family members, only 9 protein kinases outside of the HER family are inhibited by >80% at 10 uM in a broad panel of >400 protein and lipid kinases.
MTX-531 demonstrates concentration-dependent inhibition of EGFR, PI3K and mTOR as measured by lower levels of phosphorylated (p)EGFR, protein kinase B (Akt) and eukaryotic translation initiation factor 4E-binding protein 1 (4E-BP1) in CAL-33 HNSCC model.
MTX-531 (100 mg/ kg, oral daily administration) inhibits EGFR and PI3K-mTOR signaling and tumor growth in HNSCC PDX models, potentiates MEK inhibition in CRC, and is synergistic with KRAS-G12C inhibition.
MTX-531 acts as a weak agonist of PPARγ, an attribute that likely mitigates hyperglycemia induced by PI3K inhibition.

物理化学性质&存储条件

分子量 453.95
分子式 C22H20ClN5O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-N-(2-chloro-5-(4-((1-phenylethyl)amino)quinazolin-6-yl)pyridin-3-yl)methane-sulfonamide

参考文献

1. Whitehead CE, et al. Nat Cancer. 2024 Jul 11. doi: 10.1038/s43018-024-00781-6.

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