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MTX-531

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 hyperglycemia induced by PI3K inhibitors[1].

Product Specifications

CAS Number

[2791417-66-6]

UNSPSC

12352211

Target

EGFR; PI3K; PPAR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; JAK/STAT Signaling; Metabolic Enzyme/Protease; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Vitamin D Related/Nuclear Receptor

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mtx-531.html

Purity

99.87

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

ClC1=C(NS(=O)(C)=O)C=C(C2=CC3=C(N=CN=C3N[C@@H](C4=CC=CC=C4)C)C=C2)C=N1

Molecular Formula

C22H20ClN5O2S

Molecular Weight

453.94

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; PPARγ

Available Sizes

Curated Selection

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