BIX01294 triHCl

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BIX01294 triHCl
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Cat #: V3451 CAS #: 1392399-03-9 (HCl salt) Purity ≥ 98%

Description: BIX01294 triHCl (the tri-hydrochloride salt of BIX01294) is a novel and potent inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay.

References: Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33(5):108341.

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Molecular Weight (MW)600.02
Molecular FormulaC28H38N6O2.3HCl
CAS No.1392399-03-9 (HCl salt)
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 98 mg/mL (163.3 mM)r
Water: >10 mg/mLr
Ethanol: >10 mg/mL (13.33 mM)
SMILES CodeCN1CCN(C2=NC(NC3CCN(CC4=CC=CC=C4)CC3)=C5C=C(OC)C(OC)=CC5=N2)CCC1.[H]Cl.[H]Cl.[H]Cl
SynonymsBIX01294; BIX-01294; BIX 01294; N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine trihydrochloride
ProtocolIn VitroBIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride. BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells. BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines. BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLK. BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth.
In VivoBIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited.
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
1mM1.6666 mL8.3331 mL16.6661 mL33.3322 mL
5mM0.3333 mL1.6666 mL3.3332 mL6.6664 mL
10mM0.1667 mL0.8333 mL1.6666 mL3.3332 mL
20mM0.0833 mL0.4167 mL0.8333 mL1.6666 mL
Quality Control Documentation
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)
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Volume(start)
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Concentration(final)
C2
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Volume(final)
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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.