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BRM/BRG1 ATP Inhibitor-1

Cat. No. M10668
BRM/BRG1 ATP Inhibitor-1 Structure
Synonym:

ABM-879177

Size Price Availability Quantity
1mg USD 560  USD560 In stock
5mg USD 890  USD890 In stock
10mg USD 1330  USD1330 In stock
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Quality Control & Documentation
Biological Activity

BRM/BRG1 ATP Inhibitor-1 is an orally active inhibitor (IC50 below 5 nM) of Brahma Homolog (BRM)/SMARCA2 ATPase activity for the treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant cancers.

Chemical Information
Molecular Weight 318.27
Formula C11H9F3N4O2S
CAS Number 2270879-17-7
Solubility (25°C) DMSO ≥ 100 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] Julien P N Papillon, et al. J Med Chem . Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers

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Keywords: BRM/BRG1 ATP Inhibitor-1, ABM-879177 supplier, Epigenetic Reader Domain, inhibitors, activators


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