An EGFR antagonist and PI3K inhibitor
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MTX-531

Item No. 43038

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-chloro-5-[4-[[(1R)-1-phenylethyl]amino]-6-quinazolinyl]-3-pyridinyl]-methanesulfonamide
CAS Number
2791417-66-6
Molecular Formula
C22H20ClN5O2S
Formula Weight
453.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
C[C@H](C1=CC=CC=C1)NC2=NC=NC3=C2C=C(C4=CN=C(Cl)C(NS(C)(=O)=O)=C4)C=C3
InChi Code
InChI=1S/C22H20ClN5O2S/c1-14(15-6-4-3-5-7-15)27-22-18-10-16(8-9-19(18)25-13-26-22)17-11-20(21(23)24-12-17)28-31(2,29)30/h3-14,28H,1-2H3,(H,25,26,27)/t14-/m1/s1
InChi Key
LPJIZDSOUGHTNB-CQSZACIVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $207

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    25 mg

    $491

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    Product Description

    MTX-531 is an EGFR antagonist and PI3K inhibitor.1 It selectively inhibits EGFR over HER2 and HER4 (IC50s = 14.7, 2,500, and >10,000 nM, respectively) and PI3Kδ, PI3Kα, and PI3Kγ over PI3Kβ (IC50s = 1.1, 6.4, 8.3, and 233 nM, respectively) but also inhibits DNA-dependent protein kinase (DNA-PK; IC50s = 5.4 nM). MTX-531 also induces gene expression in a reporter assay using HEK293 cells expressing PPARγ (EC50 = 3.4 µM). It decreases phosphorylated levels of Akt and 4E-BP1 and induces apoptosis in CAL-33 tongue squamous cell carcinoma cells when used at concentrations ranging from 3 to 10 µM. MTX-531 (100 mg/kg per day) reduces tumor volume and increases survival in a CAL-33 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Whitehead , C.E., Ziemke, E.K., Frankowski-McGregor, C., et al. A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. Nat. Cancer 5(8), 1250-1266 (2024).