HPK1-IN-2 dihydrochloride

Name: HPK1-IN-2 dihydrochloride
Brand: MedChemExpress
SKU: HY-132150A
Rating: 4.5 (0 reviews)

Cat. No.: HY-132150A: Ficha de datos
COA

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HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC₅₀<0.05 μΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 μΜ<IC₅₀<0.5 μΜ) and Flt3 (IC₅₀<0.05 μΜ) kinase activities.

Para uso exclusivo en investigación. No vendemos a pacientes.

HPK1-IN-2 dihydrochloride Estructura química

No. CAS : 2375595-72-3

Tamaño	Stock	Cantidad
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 1 Customer Validation

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas MAP4K:

Ver todas las isoformas

MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

Ver todos los productos específicos de isoformas Src:

Ver todas las isoformas

Lck Fyn Blk Fgr Hck Lyn Yes Csk SRC-3

Actividad biológica
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

IC₅₀ & Target

IC50: <0.05 µΜ (HPK1); <0.05 µΜ (Flt3); 0.05-0.5 µΜ (Lck)^[1]

In Vitro

In a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 (example A1) dihydrochloride inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC₅₀ values of 0.3-1 μΜ and >3μΜ, respectively^[1].

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

In Vivo

HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) dihydrochloride treatment shows a dose-dependently tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumour growth by 44% and 64%, respectively^[1].

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

Animal Model:	Female BALB/c mice (6-8week old) injected with CT26 cancer cells^[1]
Dosage:	75 mg/kg and 150 mg/kg
Administration:	Oral gavage; daily; for 21 days
Result:	Showed a dose-dependently tumor growth inhibition.

Peso molecular

453.39

Fòrmula

C₁₉H₂₂Cl₂N₆OS

No. CAS

2375595-72-3

Appearance

Solid

Color

Light brown to brown

SMILES

O=C1C(C2=NC3=CC=C(N4CCN(C)CC4)C=C3N2)=C(N)C(C=CS5)=C5N1.[H]Cl.[H]Cl

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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)

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (220.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (55.14 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2056 mL	11.0280 mL	22.0561 mL
5 mM	0.4411 mL	2.2056 mL	4.4112 mL
10 mM	0.2206 mL	1.1028 mL	2.2056 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.

Calculadora de molaridad
Calculadora de dilución

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: ≥ 2.5 mg/mL (5.51 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 (5.51 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.

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).

Pureza y Documentación

Purity: 97.09%

Select Batch:

Ficha de datos (274 KB) SDS (252 KB)

COA (250 KB) HNMR (294 KB) RP-HPLC (252 KB) MS (69 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Peter Brent Sampson, et al. Hpk1 inhibitors and methods of using same. WO2016205942A1.

[2]. Mark R. Bray, et al. Salt and crystal forms of 4-amino-5-(6-(4-methylpiperazin-1-yl)-1h-benzo[d]imidazol-2-yl)thieno[2,3-b]pyridin-6(7h)-one. WO2021226707A1.

Complete Stock Solution Preparation Table

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

H₂O / DMSO	1 mM	2.2056 mL	11.0280 mL	22.0561 mL	55.1402 mL
	5 mM	0.4411 mL	2.2056 mL	4.4112 mL	11.0280 mL
	10 mM	0.2206 mL	1.1028 mL	2.2056 mL	5.5140 mL
	15 mM	0.1470 mL	0.7352 mL	1.4704 mL	3.6760 mL
	20 mM	0.1103 mL	0.5514 mL	1.1028 mL	2.7570 mL
	25 mM	0.0882 mL	0.4411 mL	0.8822 mL	2.2056 mL
	30 mM	0.0735 mL	0.3676 mL	0.7352 mL	1.8380 mL
	40 mM	0.0551 mL	0.2757 mL	0.5514 mL	1.3785 mL
	50 mM	0.0441 mL	0.2206 mL	0.4411 mL	1.1028 mL
DMSO	60 mM	0.0368 mL	0.1838 mL	0.3676 mL	0.9190 mL
	80 mM	0.0276 mL	0.1379 mL	0.2757 mL	0.6893 mL
	100 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5514 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.