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PROTAC SOS1 degrader-4

Cat. No. M43462
PROTAC SOS1 degrader-4 Structure
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Biological Activity

PROTAC SOS1 degrader-4 is a potent SOS1 degrader.

Chemical Information
Molecular Weight 993.65
Formula C53H65ClN8O7S
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] Tingkai Chen et al. Eur J Med Chem. Inhibition of Son of Sevenless Homologue 1 (SOS1): Promising therapeutic treatment for KRAS-mutant cancers

[2] Sajid Khan et al. Adv Cancer Res. Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies

[3] Gerhard Hamilton et al. Curr Pharm Des. Targeting of SOS1: from SOS1 Activators to Proteolysis Targeting Chimeras

[4] Zehui Zhou et al. J Med Chem. Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers

[5] Yujia Bian et al. J Med Chem. Development of SOS1 Inhibitor-Based Degraders to Target KRAS-Mutant Colorectal Cancer

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Keywords: PROTAC SOS1 degrader-4 supplier, PROTAC, inhibitors, activators


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