An inhibitor of mutant EGFRs
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Alflutinib (mesylate)

Item No. 31473

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[[2-(dimethylamino)ethyl]methylamino]-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]-6-(2,2,2-trifluoroethoxy)-3-pyridinyl]-2-propenamide, monomethanesulfonate
CAS Number
2130958-55-1
Synonyms
  • AST2818
Molecular Formula
C28H31F3N8O2 • CH3SO3H
Formula Weight
664.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 10 mg/mlDMF: slightly solubleDMSO: slightly soluble
λmax
267, 332 nm
SMILES
O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(OCC(F)(F)F)N=C1N(CCN(C)C)C)C=C.O=S(O)(C)=O
InChi Code
InChI=1S/C28H31F3N8O2.CH4O3S/c1-6-24(40)33-21-15-22(26(41-17-28(29,30)31)36-25(21)38(4)14-13-37(2)3)35-27-32-12-11-20(34-27)19-16-39(5)23-10-8-7-9-18(19)23;1-5(2,3)4/h6-12,15-16H,1,13-14,17H2,2-5H3,(H,33,40)(H,32,34,35);1H3,(H,2,3,4)
InChi Key
WDPGHXINXNBHAS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    Product Description

    Aflutinib is an inhibitor of mutant EGFRs.1 It is selective for EGFRL858R, EGFRG719X, EGFRL858R, EGFRL861A, and EGFRT790M mutant EGFRs over wild-type EGFR. Aflutinib (10 and 30 mg/kg) reduces tumor growth in an EGFRL858R and EGFRT790M-expressing LU1868 non-small cell lung cancer (NSCLC) patient-derived xenograft (PDX) mouse model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shi, Y., Zhang, S., Hu, X., et al. Safety, clinical activity, and pharmacokinetics of alflutinib (AST2818) in patients with advanced NSCLC with EGFR T790M mutation. J. Thorac. Oncol. 15(6), 1015-1026 (2020).