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Sunvozertinib

Cat. No. M11447
Sunvozertinib Structure
Synonym:

DZD9008

Size Price Availability
5mg USD 480  USD480 4-7 Days
10mg USD 800  USD800 4-7 Days
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Quality Control & Documentation
Biological Activity

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).

Chemical Information
Molecular Weight 584.08
Formula C29H35ClFN7O3
CAS Number 2370013-12-8
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Mengzhao Wang, et al. Cancer Discov. Sunvozertinib, a selective EGFR inhibitor for previously treated non-small cell lung cancer with EGFR exon 20 insertion mutations

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Keywords: Sunvozertinib, DZD9008 supplier, EGFR/HER2, inhibitors, activators

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