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PROTAC RAF degrader 1

Cat. No. M43467
PROTAC RAF degrader 1 Structure
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Biological Activity

PROTAC RAF degrader 1 is a PROTAC RAF degrader.

Chemical Information
Molecular Weight 1010.18
Formula C51H57F2N9O7S2
CAS Number 2413035-41-1
Form Solid
Solubility (25°C) DMSO 130 mg/mL (Need ultrasonic)
Storage 4°C, protect from light
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] Ru Si et al. Bioorg Med Chem Lett. Discovery of novel PROTACs based on multi-targeted angiogenesis inhibitors

[2] Yihui Song et al. Pharmacol Ther. Double-edged roles of protein tyrosine phosphatase SHP2 in cancer and its inhibitors in clinical trials

[3] Chao Wang et al. Eur J Med Chem. Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer

[4] Shanique Alabi et al. Nat Commun. Mutant-selective degradation by BRAF-targeting PROTACs

[5] Hong Chen et al. Bioorg Chem. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation

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Keywords: PROTAC RAF degrader 1 supplier, Raf, inhibitors, activators


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