A selective estrogen receptor covalent antagonist
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H3B-5942

Item No. 31454

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-4-[[2-[4-[(1E)-1-(1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]amino]-N,N-dimethyl-2-butenamide
CAS Number
2052128-15-9
Molecular Formula
C31H34N4O2
Formula Weight
494.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 1 mg/mlEthanol: 5 mg/ml
λmax
236 nm
SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCNC/C=C/C(N(C)C)=O)\C3=CC=C(NN=C4)C4=C3
InChi Code
InChI=1S/C31H34N4O2/c1-4-28(23-9-6-5-7-10-23)31(25-14-17-29-26(21-25)22-33-34-29)24-12-15-27(16-13-24)37-20-19-32-18-8-11-30(36)35(2)3/h5-17,21-22,32H,4,18-20H2,1-3H3,(H,33,34)/b11-8+,31-28+
InChi Key
BYAUIDXIQATDBT-GIHLFXONSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    H3B-5942 is a selective estrogen receptor covalent antagonist (SERCA).1 It covalently modifies cysteine 530 in the ligand binding domain of wild-type estrogen receptor α (ERα) and ERαY537S. HB-5942 inhibits expression of the ERα target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ERα (IC50s = 2.74 and 1.3 nM, respectively) or the mutant receptors ERαY537S (IC50s = 29.38 and 19.4 nM, respectively), ERαY537N (IC50s = 8.14 and 6.1 nM, respectively), ERαY537C (IC50s = 12.19 and 9.5 nM, respectively), or ERαD538G (IC50s = 24.87 and 4 nM, respectively), which are active independent of estradiol. It inhibits the growth of MCF-7 cells overexpressing wild-type ERα or ERαY537S (GI50s = 1.3 and 8.3 nM, respectively). H3B-5942 reduces tumor growth in an MCF-7 mouse xenograft model and an ERαY537S/WT ST941 patient-derived xenograft (PDX) mouse model in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Puyang, X., Furman, C., Zheng, G.Z., et al. Discovery of selective estrogen receptor covalent antagonists for the treatment of ERαWT and ERαMUT breast cancer. Cancer Discov. 8(9), 1176-1193 (2018).