Sunvozertinib (DZD9008) is an effective inhibitor of ErbBs (EGFR, Her2, especially mutants) and BTK. Sunvozertinib showed EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and IC50 of Her2 exon 20 YVMA and EGFR WT A431 They are 20.4, 20.4, 1.1, 7.5 and 80.4 nM respectively (please refer to patent WO2019149164A1, Example 52 for details).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
|Related EGFR/HER2 Products|
Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR).
(S)-Sunvozertinib ((S)-DZD9008) is the S-enantiomer of Sunvozertinib, EGFR exon 20 NPH and ASV insertion, EGFR L858R/T790M mutation and Her2 exon 20 YVMA insertion (IC50 was 51.2 nM, 51.9 nM, 1 nM and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
(Rac)-JBJ-04-125-02 is a racemate of JBJ-04-125-02, which is a potent, selectively mutated, allosteric and oral active EGFR inhibitor. The IC50 of EGFRL858R/T790M was 0.26 nM.
AZ7550 Mesylate is an active metabolite of AZD9291, AZ7550 inhibits IGF1R activity,IC50 1.6 μM.
TAS0728 is an effective, selective, oral, irreversible, covalently bound HER2 inhibitor covalently bound to the C805 site of HER2, inhibiting its activity.IC50 The value is 13 nM. TAS0728 to BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and HUMAN HER2 IC50 The values are 4.9, 8.5, 31, 65, 33, 25, 86, and 36 nM, respectively. TAS0728 simultaneously inhibits phosphorylation of HER2, HER3 and its downstream effector proteins. Has antitumor activity.
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