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B-Raf inhibitor 1

Cat. No. M9492
B-Raf inhibitor 1 Structure
Synonym:

ABM-0403

Size Price Availability Quantity
5mg USD 110  USD110 In stock
10mg USD 175  USD175 In stock
50mg USD 630  USD630 In stock
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Quality Control & Documentation
Biological Activity

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 µM and 2 nM for A375 proliferation and A375 p-ERK, respectively. B-Raf inhibitor 1 inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-Raf inhibitor 1 additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers.

Chemical Information
Molecular Weight 478.94
Formula C26H19ClN8
CAS Number 1093100-40-3
Solubility (25°C) DMSO ≥ 50 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] Shanique Alabi, et al. Mutant-selective degradation by BRAF-targeting PROTACs

[2] Arunkumar Babu, et al. A Fluoro Derivative of Embelin, as Potent B-RAF Inhibitor in Melanoma

[3] Eunyoung Park, et al. Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes

[4] E M L Heath, et al. B-RAF: A contributor to the melanoma phenotype

[5] Gideon Bollag, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

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  Catalog
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Keywords: B-Raf inhibitor 1, ABM-0403 supplier, Raf, inhibitors, activators


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