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iHCK-37

Chemical Structure : iHCK-37

CAS No.: 516478-09-4

iHCK-37 (ASN05260065)

Catalog No.: PC-72678Not For Human Use, Lab Use Only.

iHCK-37 (ASN05260065) is a potent and selective Hck inhibitor with Ki of 0.22 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

iHCK-37 (ASN05260065) is a potent and selective Hck inhibitor with Ki of 0.22 uM.
iHCK-37 displays high selectivity against a panel of kinases including other Src family members (Blk, Fgr, Fyn, cSRC, Lck, Lyn, Syk, and Yes), tyrosine kinases (Abl and Abl-T315I), as well as some kinases important for HIV1 (CDK9, FAK, Itk, JAK3, Ron).
iHCK-37 has anti-neoplastic activity in leukemia cells without altering apoptosis and survival rate of normal cells.
iHCK-37 demonstrates additive effects against leukemia cells combined with 5-Azacytidine or Cytarabine, reduces the activation of oncogenic pathways, MAPK/ERK and PI3K/AKT, leading to reduction of ERK and AKT phosphorylation, and increases BAX and decreased BCL-XL protein expression.
iHCK-37 exhibits antiproliferative activity profile against the human leukemia cell line KU-812 (IC50=66.5 uM).
iHCK-37 also blocks HIV-1 replication with EC50 of 12.9 uM.

Physicochemical Properties

M.Wt 544.73
Formula C30H32N4O2S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-[2-(4-Morpholinyl)phenyl]-2-[[5,6,7,8-tetrahydro-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]thio]acetamide

References

1. Roversi FM, et al. Biochim Biophys Acta Mol Basis Dis. 2017 Feb;1863(2):450-461.

2. Roversi FM, et al. Cancer Immunol Immunother. 2022 Jan 18.

3. Cristina Tintori, et al. ChemMedChem. 2013 Aug;8(8):1353-60.

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