2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. H3B-5942

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations.

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H3B-5942

H3B-5942 화학구조

CAS No. : 2052128-15-9

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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H3B-5942 Related Antibodies

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View All Estrogen Receptor/ERR Isoform Specific Products:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations[1].

IC50 & Target[1]

ERαY537S

0.41 nM (Ki)

ERαWT

1 nM (Ki)

In Vitro

H3B-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[1].
H3B-5942 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line[1].
H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERαWT or clinically frequent ERα mutations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

H3B-5942 Related Antibodies
In Vivo

H3B-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[1].
H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERαY537S/WT ST941 model in athymic female nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCF7 xenograft model in athymic female nude mice[1]
Dosage: 1, 3, 10, or 30 mg/kg
Administration: P.O. once a day (q.d.×1) for 17 days
Result: Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.
분자량

494.63

화학식

C31H34N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : 83.33 mg/mL (168.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0217 mL 10.1086 mL 20.2171 mL
5 mM 0.4043 mL 2.0217 mL 4.0434 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서

Purity: 98.25%

SDS (393 KB)

COA (245 KB) HNMR (384 KB) RP-HPLC (259 KB) LCMS (101 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0217 mL 10.1086 mL 20.2171 mL 50.5428 mL
5 mM 0.4043 mL 2.0217 mL 4.0434 mL 10.1086 mL
10 mM 0.2022 mL 1.0109 mL 2.0217 mL 5.0543 mL
15 mM 0.1348 mL 0.6739 mL 1.3478 mL 3.3695 mL
20 mM 0.1011 mL 0.5054 mL 1.0109 mL 2.5271 mL
25 mM 0.0809 mL 0.4043 mL 0.8087 mL 2.0217 mL
30 mM 0.0674 mL 0.3370 mL 0.6739 mL 1.6848 mL
40 mM 0.0505 mL 0.2527 mL 0.5054 mL 1.2636 mL
50 mM 0.0404 mL 0.2022 mL 0.4043 mL 1.0109 mL
60 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8424 mL
80 mM 0.0253 mL 0.1264 mL 0.2527 mL 0.6318 mL
100 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5054 mL
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H3B-5942 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H3B-59422052128-15-9Estrogen Receptor/ERRInhibitorinhibitorinhibit

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상품명:
H3B-5942
Cat. No.:
HY-112611
수량:
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SAFETY DATA SHEET (SDS)

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