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HPK1-IN-2 dihydrochloride

Catalog No.GC73012

HPK1-IN-2 didrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity.

Products are for research use only. Not for human use. We do not sell to patients.

HPK1-IN-2 dihydrochloride Chemical Structure

Cas No.: 2375595-72-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$228.00
In stock
5 mg
$207.00
In stock
10 mg
$351.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of HPK1-IN-2 dihydrochloride

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

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

HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) 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].

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

Chemical Properties of HPK1-IN-2 dihydrochloride

Cas No. 2375595-72-3 SDF
Formula C19H22Cl2N6OS M.Wt 453.39
Solubility DMSO : 100 mg/mL (220.56 mM; Need ultrasonic); H2O : 25 mg/mL (55.14 mM; Need ultrasonic) Storage 4°C, sealed storage, away from moisture and light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of HPK1-IN-2 dihydrochloride

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1 mg 5 mg 10 mg
1 mM 2.2056 mL 11.028 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
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In vivo Formulation Calculator (Clear solution) of HPK1-IN-2 dihydrochloride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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