STAT3-SH2 domain inhibitor 1

Name: STAT3-SH2 domain inhibitor 1
Brand: MedChemExpress
SKU: HY-151577
Rating: 4.5 (0 reviews)

Cat. No.: HY-151577 Purity: 98.58%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a K_d value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.

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STAT3-SH2 domain inhibitor 1 화학구조

CAS No. : 2816059-41-1

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 Customer Validation

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	1.54 μM Compound: 7; W1046	Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36170649]
H9c2	IC₅₀	9.05 μM Compound: 7; W1046	Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36170649]
MGC-803	IC₅₀	4.73 μM Compound: 7; W1046	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 36170649]

In Vitro

STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway^[1].
STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC₅₀ values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively^[1].
STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	AGS and MGC-803 cell lines
Concentration:	0-10 μM
Incubation Time:	72 hours
Result:	Suppressed cancer cell proliferation and growth.

Apoptosis Analysis^[1]

Cell Line:	AGS and MGC-803 cell lines
Concentration:	1 and 3 μM
Incubation Time:	72 hours
Result:	Induced apoptosis in AGS cells in a concentration-dependent manner, resulting in apoptotic percentages of 13.0 and 26.7% at 1 and 3 μM, respectively. Induced apoptosis of MGC-803 cells in a dose-dependent way, leading to apoptotic percentage of 11.2% at 5 μM.

Western Blot Analysis^[1]

Cell Line:	AGS and MGC-803 cell lines
Concentration:	1 and 3 μM
Incubation Time:	24 hours
Result:	Inhibited STAT3 phosphorylation at Tyr705 in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	HEK-293T cells
Concentration:	1, 3, and 5 μM
Incubation Time:	24 hours
Result:	Disrupted STAT3 dimerization in HEK-293T cells.

In Vivo

STAT3-SH2 domain inhibitor 1 (compound 7; 5 and 15 mg/kg; i.p.; daily, for 20 d) exhibits superior antitumor activity in BALB/c male nude mice with gastric tumor xenografts^[1].

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

Animal Model:	BALB/c male nude mice with gastric tumor xenografts^[1]
Dosage:	5 and 15 mg/kg
Administration:	Intraperitoneal injection; daily, for 20 days
Result:	Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of 65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively.

분자량

610.40

화학식

C₂₈H₂₈BF₅N₂O₅S

CAS No.

2816059-41-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C1=CC=C(B(O)O)C=C1)CC2=CC=C(C3CCCCC3)C=C2)CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 8.33 mg/mL (13.65 mM; ultrasonic and warming and heat to 80°C; 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	1.6383 mL	8.1913 mL	16.3827 mL
5 mM	0.3277 mL	1.6383 mL	3.2765 mL
10 mM	0.1638 mL	0.8191 mL	1.6383 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 0.83 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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% (20% SBE-β-CD in Saline)
Solubility: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 0.83 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 0.83 mg/mL. 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 (8.3 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)

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: 98.58%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (250 KB) HNMR (149 KB) RP-HPLC (247 KB) LCMS (380 KB)

Handling Instructions (2659 KB)

References

[1]. Deng L, et, al. Boronic Acid: A Novel Pharmacophore Targeting Src Homology 2 (SH2) Domain of STAT3. J Med Chem. 2022 Oct 13;65(19):13094-13111. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6383 mL	8.1913 mL	16.3827 mL	40.9567 mL
	5 mM	0.3277 mL	1.6383 mL	3.2765 mL	8.1913 mL
	10 mM	0.1638 mL	0.8191 mL	1.6383 mL	4.0957 mL