GSK143 dihydrochloride

Name: GSK143 dihydrochloride
Brand: MedChemExpress
SKU: HY-12736A
Rating: 4.5 (1 reviews)

Cat. No.: HY-12736A Purity: 99.73%: FAQs
Data Sheet SDS COA Handling Instructions

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GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

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GSK143 dihydrochloride Chemical Structure

CAS No. : 2341796-81-2

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 230	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 920	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1550	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of GSK143 dihydrochloride:

GSK143 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1)^[1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice^[2]^[3].

IC₅₀ & Target

pIC50: 7.5 (SYK) and 7.1 (pErk)^[1]

In Vitro

GSK143 dihydrochloride (compound 20) inhibits ZAP-70 (pIC₅₀=4.7), LCK (pIC₅₀=5.3), LYN (pIC₅₀=5.4), JAK1/2/3 (pIC₅₀=5.8/5.8/5.7), Aurora B (pIC₅₀=4.8), hWB (pIC₅₀=6.6), hERG (pIC₅₀=4.7)^[1].
GSK143 dihydrochloride (10-10000 nM; every 24 hours for 3 days) has an IC₅₀ of 323 nM in CLL cells. GSK 143 dihydrochloride (1 μM; 30 mins) abrogates early signalling events including SYK phosphorylation and calcium flux^[2].
GSK143 dihydrochloride (0.1-10 μM; for 30 min) reduces cytokine expression in bone marrow derived macrophages in a concentration-dependent manner^[3].

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

Cell Viability Assay^[2]

Cell Line:	Chronic lymphocytic leukaemia (CLL) cells
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:	Every 24 hours for 3 days
Result:	Had an IC₅₀ of 323 nM.

In Vivo

GSK143 (0.1-10 mg/kg; orally; 1.5 hours) reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis of 1 mg/kg^[3].
GSK143 (3, 10, 30, 100 mg/kg; oral; 1 hour before ovalbumin challenge) reduces the cutaneous reverse passive Arthus reaction in a dose dependent manner by approximately 50% and 70% at 10 mg/kg and 30 mg/kg, respectively^[2].
GSK143 (iv of 1 mg/kg; po of 3 mg/kg) has a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg in rats^[1].

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

Animal Model:	Wild type C57NL/BL6 mice, 10-12 weeks old^[3]
Dosage:	0.1, 1, 3, 10 mg/kg
Administration:	Orally; 1.5 hours before intestinal manipulation (IM)
Result:	Reduced inflammation and prevented recruitment of immune cells in the intestinal muscularis.

Animal Model:	Male CD rats (175-200 g)^[1]
Dosage:	1 mg/kg of iv; 3 mg/kg of po (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 4.2 hours, low clearance (16 mL/min/kg), moderate bioavailability of 30% and a V_ss of 4.1 L/kg.

Molecular Weight

415.32

Formula

C₁₇H₂₄Cl₂N₆O₂

CAS No.

2341796-81-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

[H]Cl.[H]Cl.O=C(C1=CN=C(N[C@H]2[C@@H](N)COCC2)N=C1NC3=CC=C(C)C=C3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (240.78 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (120.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4078 mL	12.0389 mL	24.0778 mL
5 mM	0.4816 mL	2.4078 mL	4.8156 mL
10 mM	0.2408 mL	1.2039 mL	2.4078 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.73%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (253 KB) HNMR (272 KB) RP-HPLC (244 KB) MS (73 KB)

Handling Instructions (2659 KB)

References

[1]. John Liddle, et al. Discovery of GSK143, a Highly Potent, Selective and Orally Efficacious Spleen Tyrosine Kinase Inhibitor. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. [Content Brief]

[2]. Abraham M Varghese, et al. Highly Selective SYK Inhibitor, GSK143, Abrogates Survival Signals in Chronic Lymphocytic Leukaemia. Br J Haematol. 2018 Sep;182(6):927-930. [Content Brief]

[3]. Sjoerd H W van Bree, et al. Inhibition of Spleen Tyrosine Kinase as Treatment of Postoperative Ileus. Gut. 2013 Nov;62(11):1581-90. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	2.4078 mL	12.0389 mL	24.0778 mL	60.1945 mL
	5 mM	0.4816 mL	2.4078 mL	4.8156 mL	12.0389 mL
	10 mM	0.2408 mL	1.2039 mL	2.4078 mL	6.0195 mL
	15 mM	0.1605 mL	0.8026 mL	1.6052 mL	4.0130 mL
	20 mM	0.1204 mL	0.6019 mL	1.2039 mL	3.0097 mL
	25 mM	0.0963 mL	0.4816 mL	0.9631 mL	2.4078 mL
	30 mM	0.0803 mL	0.4013 mL	0.8026 mL	2.0065 mL
	40 mM	0.0602 mL	0.3010 mL	0.6019 mL	1.5049 mL
	50 mM	0.0482 mL	0.2408 mL	0.4816 mL	1.2039 mL
	60 mM	0.0401 mL	0.2006 mL	0.4013 mL	1.0032 mL
	80 mM	0.0301 mL	0.1505 mL	0.3010 mL	0.7524 mL
	100 mM	0.0241 mL	0.1204 mL	0.2408 mL	0.6019 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.