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HPK1-IN-2

Catalog No. T9017   CAS 2056122-11-1
Synonyms: Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2, HPK1-IN-2

HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1; IC50<0.05 μΜ). It also inhibits Lck (0.05 μΜ<IC50<0.5 μΜ) and Flt3 (IC50<0.05 μΜ) kinase activities with antitumor activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
HPK1-IN-2 Chemical Structure
HPK1-IN-2, CAS 2056122-11-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 118.00
5 mg In stock $ 243.00
10 mg In stock $ 405.00
25 mg In stock $ 676.00
50 mg In stock $ 962.00
100 mg In stock $ 1,280.00
500 mg In stock $ 2,590.00
1 mL * 10 mM (in DMSO) In stock $ 289.00
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Purity: 98.4%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description HPK1-IN-2 (Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2) is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1; IC50<0.05 μΜ). It also inhibits Lck (0.05 μΜ<IC50<0.5 μΜ) and Flt3 (IC50<0.05 μΜ) kinase activities with antitumor activity.
Targets&IC50 FLT3:<0.05 µΜ , HPK1:IC50<0.05 µΜ, Lck:0.05 µΜ<IC50<0.5 µΜ
In vitro In a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 μΜ and >3μΜ, respectively.
In vivo HPK1-IN-2 (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
Synonyms Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2, HPK1-IN-2
Molecular Weight 380.47
Formula C19H20N6OS
CAS No. 2056122-11-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 25 mg/mL (55.14 mM), Sonication is recommended.

TargetMolReferences and Literature

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

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Compound Library Angiogenesis related Compound Library Bioactive Compound Library Bioactive Compounds Library Max Orally Active Compound Library Anti-Cancer Metabolism Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

HPK1-IN-2 2056122-11-1 Angiogenesis Others Tyrosine Kinase/Adaptors FLT Src Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2 HPK1 IN 2 dihydrochloride HPK-1-IN-2 dihydrochloride HPK1IN2 dihydrochloride inhibitor inhibit

 

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