An inhibitor of EGFR ex20ins
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Enantiomer(s)
38900​(S)-Sunvozertinib
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Sunvozertinib

Item No. 46085

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-[[4-[[5-chloro-4-fluoro-2-(1-hydroxy-1-methylethyl)phenyl]amino]-2-pyrimidinyl]amino]-2-[(3R)-3-(dimethylamino)-1-pyrrolidinyl]-4-methoxyphenyl]-2-propenamide
CAS Number
2370013-12-8
Synonyms
  • DZD9008
Molecular Formula
C29H35ClFN7O3
Formula Weight
584.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
C=CC(NC1=C(N2CC[C@H](C2)N(C)C)C=C(C(NC3=NC=CC(NC4=C(C(C)(C)O)C=C(F)C(Cl)=C4)=N3)=C1)OC)=O
InChi Code
InChI=1S/C29H35ClFN7O3/c1-7-27(39)34-22-14-23(25(41-6)15-24(22)38-11-9-17(16-38)37(4)5)35-28-32-10-8-26(36-28)33-21-13-19(30)20(31)12-18(21)29(2,3)40/h7-8,10,12-15,17,40H,1,9,11,16H2,2-6H3,(H,34,39)(H2,32,33,35,36)/t17-/m1/s1
InChi Key
BTMKEDDEMKKSEF-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

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    Product Description

    Sunvozertinib is an irreversible inhibitor of EGFR containing exon 20 insertion (ex20ins) mutations (IC50 = 2.1 nM for EGFR ex20ins 770_NPG).1 It is selective for EGFR ex20ins and EGFRL858R/T790M (IC50 = 13 nM) over wild-type EGFR, HER2, and HER4 (IC50s = 226, 392, and 704 nM, respectively), a panel of 106 kinases at 1 µM, and other kinases, including BTK, BRK, ALK, Yes, and TrkA (IC50s = 213, 529, 1,172, 2,895, and >10,000 nM, respectively). Sunvozertinib selectively inhibits the proliferation of mutant EGFR-expressing cancer cells (GI50s = 6-88 nM) over those containing wild-type EGFR (GI50 = 113 nM). Sunvozertinib (25 and 50 mg/kg twice per day) induces tumor regression in a patient-derived xenograft (PDX) mouse model of non-small cell lung cancer (NSCLC) carrying EGFR ex20ins insNPH. Formulations containing sunvozertinib have been used in the treatment of NSCLC with EGFR ex20ins mutations.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, M., Yang, J.C., Mitchell, P.L., et al. Sunvozertinib, a selective EGFR inhibitor for previously treated non-small cell lung cancer with EGFR Exon 20 insertion mutations. Cancer Discov. 12(7), 1676-1689 (2022).