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DBPR112 HCl

CAT: 0931-T69498-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0931-T69498-01Size:25 mg
Selected
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
2889316-21-4
Target
Others
Related Pathways
Others
Bioactivity
DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib, against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.
Smiles
N([C@H](CO)C1=CC=CC=C1)C2=C3C(=C(OC3=NC=N2)C4=CC=CC=C4)C5=CC(NC(/C=C/CN(C)C)=O)=CC=C5.Cl
Molecular Formula
C32H32ClN5O3
Molecular Weight
570.08
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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