An inhibitor of mutant EGFR
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BLU-945

Item No. 43015

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[(3S,4R)-3-fluoro-4-methoxy-1-piperidinyl]-4-pyrimidinyl]-5-(1-methylethyl)-8-[(2R,3S)-2-methyl-3-[(methylsulfonyl)methyl]-1-azetidinyl]-3-isoquinolinamine
CAS Number
2660250-10-0
Synonyms
  • Tigozertinib
Molecular Formula
C28H37FN6O3S
Formula Weight
556.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
CS(C[C@H]1CN(C2=CC=C(C(C)C)C3=C2C=NC(NC4=NC(N5CC[C@H]([C@H](C5)F)OC)=NC=C4)=C3)[C@@H]1C)(=O)=O
InChi Code
InChI=1S/C28H37FN6O3S/c1-17(2)20-6-7-24(35-14-19(18(35)3)16-39(5,36)37)22-13-31-27(12-21(20)22)32-26-8-10-30-28(33-26)34-11-9-25(38-4)23(29)15-34/h6-8,10,12-13,17-19,23,25H,9,11,14-16H2,1-5H3,(H,30,31,32,33)/t18-,19-,23+,25-/m1/s1
InChi Key
LIMFPAAAIVQRRD-BCGVJQADSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $98

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    10 mg

    $157

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    25 mg

    $270

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    50 mg

    $490

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    Product Description

    BLU-945 is an inhibitor of mutant EGFR (IC50s = 0.4 and 0.5 nM for EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively).1 It is selective for these mutants over wild-type EGFR (IC50 = 683 nM) and a panel of greater than 400 kinases at 3 µM. In vivo, BLU-945 (100 mg/kg) induces tumor regression in a mouse xenograft model using H1975 non-small cell lung cancer (NSCLC) cells, which express EGFRL858R/T790M. It inhibits tumor growth in an osimertinib-resistant patient-derived xenograft (PDX) mouse model of NSCLC using tumors harboring EGFRT790M/C797S with an exon 19 deletion.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eno, M.S., Brubaker, J.D., Campbell, J.E., et al. Discovery of BLU-945, a reversible, potent, and wild-type-sparing next-generation EGFR mutant inhibitor for treatment-resistant non-small-cell lung cancer. J. Med. Chem. 65(14), 9662-9677 (2022).