An inhibitor of EGFR and EGFRL858R/T790M
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DBPR112

Item No. 44448

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-4-(dimethylamino)-N-[3-[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-6-phenylfuro[2,3-d]pyrimidin-5-yl]phenyl]-2-butenamide
CAS Number
1226549-49-0
Synonyms
  • Gozanertinib
Molecular Formula
C32H31N5O3
Formula Weight
533.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
OC[C@H](C1=CC=CC=C1)NC2=C3C(OC(C4=CC=CC=C4)=C3C5=CC(NC(/C=C/CN(C)C)=O)=CC=C5)=NC=N2
InChi Code
InChI=1S/C32H31N5O3/c1-37(2)18-10-17-27(39)35-25-16-9-15-24(19-25)28-29-31(36-26(20-38)22-11-5-3-6-12-22)33-21-34-32(29)40-30(28)23-13-7-4-8-14-23/h3-17,19,21,26,38H,18,20H2,1-2H3,(H,35,39)(H,33,34,36)/b17-10+/t26-/m1/s1
InChi Key
NQAMTZUVRFRJCZ-VMMYIZNOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    DBPR112 is an inhibitor of EGFR and dual-mutant EGFRL858R/T790M (IC50s = 15 and 48 nM, respectively).1 It is selective for these kinases over 384 other kinases but does inhibit 11 additional kinases, including JAK3, Blk, and bone marrow tyrosine kinase on chromosome X (BMX), at 10,000 nM. DBPR112 reduces the viability of HCC827 and H1975 non-small cell lung cancer (NSCLC) cells with 50% cytotoxicity concentration values (CC50s) of 25 and 620 nM, respectively. It decreases tumor weight without affecting body weight in a HCC827 mouse xenograft model when administered at doses of 20 or 50 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lin, S.-Y., Chang Hsu, Y., Peng, Y.-H., et al. Discovery of a furanopyrimidine-based epidermal growth factor receptor inhibitor (DBPR112) as a clinical candidate for the treatment of non-small cell lung cancer. J. Med. Chem. 62(22), 10108-10123 (2019).