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Regorafenib HCl

Cat. No. M5925
Regorafenib HCl Structure
Synonym:

BAY73-4506 hydrochloride

Size Price Availability Quantity
5mg USD 38  USD38 In stock
10mg USD 60  USD60 In stock
50mg USD 120  USD120 In stock
100mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Chemical Information
Molecular Weight 519.28
Formula C21H16Cl2F4N4O3
CAS Number 835621-07-3
Solubility (25°C) 5.6 mg/mL in DMSO
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] McLellan B, et al. Ann Oncol. Regorafenib-associated hand-foot skin reaction: practical advice on diagnosis, prevention, and management.

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Keywords: Regorafenib HCl, BAY73-4506 hydrochloride supplier, VEGFR/PDGFR, inhibitors, activators


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