BRM/BRG1 ATP Inhibitor-1

This product is for research use only, not for human use. We do not sell to patients.

BRM/BRG1 ATP Inhibitor-1
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Cat #: V2478 CAS #: 2270879-17-7 Purity ≥ 99%

Description: BRM/BRG1 ATP Inhibitor-1 is an orally bioactive inhibitor of Brahma Homolog (BRM)/SMARCA2 ATPase with anticancer activity and has potential to be used for the treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.

References: Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172

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Molecular Weight (MW)318.27
Molecular FormulaC11H9F3N4O2S
CAS No.2270879-17-7
SMILES CodeO=C(NC1=CC(F)=NC=C1CO)NC2=CC(C(F)F)=NS2
SynonymsNVP-RXI570; NVP-RXI-570; NVP-RXI 570; BRM/BRG1 ATP Inhibitor-1; CUN79177; CUN79177; CUN-79177;
ProtocolIn VitroBRM/BRG1 ATP Inhibitor-1 inhibits KRT80 gene expression in H1299 cells with the AAC50 (absolute AC50) value of 0.01 μM and in RERF-LC-AI cells with an AAC50 value of 0.01 μM. BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM, 5 days) can inhibit the proliferation of cancer cells.
In VivoBRM/BRG1 ATP Inhibitor-1 (compound 14) (oral administration, 7.5 or 20 mg/kg, everyday, 3 weeks) can inhibit tumor growth and inhibit KRT80 expression in a dose-dependent manner.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM3.1420 mL15.7099 mL31.4199 mL62.8397 mL
5mM0.6284 mL3.1420 mL6.2840 mL12.5679 mL
10mM0.3142 mL1.5710 mL3.1420 mL6.2840 mL
20mM0.1571 mL0.7855 mL1.5710 mL3.1420 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.