H3B-5942

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

H3B-5942
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250mg$1850Check With Us
500mg$2600Check With Us
1g$3900Check With Us

Cat #: V31869 CAS #: 2052128-15-9 Purity ≥ 99%

Description: H3B-5942 (H3B5942) is a selective, irreversible (covalent) and orally bioavailable estrogen receptor antagonist with antitumor activity (better than fulvestrant).

References: Puyang X, et al. Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. Cancer Discov. 2018 Sep;8(9):1176-1193.

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Molecular Weight (MW)494.63
Molecular FormulaC₃₁H₃₄N₄O₂
CAS No.2052128-15-9
SMILES Code CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC/C=C/C(N(C)C)=O)C=C2)C3=CC(C=NN4)=C4C=C3
SynonymsH3B-5942; H3B 5942; H3B5942
ProtocolIn VitroH3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively.
In VivoH3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d. for 17 days) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice
Animal modelMCF7 xenograft model in athymic female nude mice
Dosages1, 3, 10, or 30 mg/kg
AdministrationP.O. once a day (q.d.×1) for 17 days
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
1mM2.0217 mL10.1086 mL20.2171 mL40.4343 mL
5mM0.4043 mL2.0217 mL4.0434 mL8.0869 mL
10mM0.2022 mL1.0109 mL2.0217 mL4.0434 mL
20mM0.1011 mL0.5054 mL1.0109 mL2.0217 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
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.