MTX-531

• 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 hyperglycemia induced by PI3K inhibitors[1].

• 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

• CAS Number:

  2791417-66-6