HPK1-IN-2

SKU: orb1298443

Description

HPK1-IN-2 is a potent, orally bioavailable small molecule inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1), also inhibiting Lck and Flt3. It demonstrates antitumor activity and is a valuable chemical probe for researching HPK1 signaling in immunology and oncology, applicable in both in vitro and in vivo experimental models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2056122-11-1
• MW: 380.47
• Purity: 99.62%
• Formula: C₁₉H₂₀N₆OS
• SMILES: NC1=C(C=2NC=3C(N2)=CC=C(C3)N4CCN(C)CC4)C(=O)NC5=C1C=CS5
• Target: Src,FLT
• Solubility: H2O:25 mg/mL (65.71 mM)

Bioactivity

• Target IC50:
  FLT3:<0.05 µΜ |HPK1:IC50<0.05 µΜ|Lck:0.05 µΜ
• 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
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Thieno[2,3-b]pyridin-6(7H)-one, 4-amino-5-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-HPK1-IN-2, HPK1, HPK1 IN 2 dihydrochloride, HPK1-IN-2, HPK1-IN-2, HPK1IN2 dihydrochloride, HPK-1-IN-2 dihydrochloride, Lck, Flt3

Compound Identifiers

PubChem CID

137297852