| Identification | Back Directory | [Name]
Acetamide, N-[2-(4-morpholinyl)phenyl]-2-[[5,6,7,8-tetrahydro-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]thio]- | [CAS]
516478-09-4 | [Synonyms]
iHCK-37
ASN05260065
Acetamide, N-[2-(4-morpholinyl)phenyl]-2-[[5,6,7,8-tetrahydro-2-(2-phenylethyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]thio]- | [Molecular Formula]
C30H32N4O2S2 | [MOL File]
516478-09-4.mol | [Molecular Weight]
544.73 |
| Chemical Properties | Back Directory | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 275 mg/mL (504.84 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.59±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research[1].
iHCK-37 (5.0-20 μM; 24 hours) exhibits a potent in vitro antiproliferative activity. The dose (μM) for growth inhibition (GI50) is 5.0-5.8 μM for AML cell lines (HL60, KG1a and U937) and 9.1-19.2 μM for chronic myeloid leukemia cell lines (HEL and K562)[2].iHCK-37 (3-9 μM; plus Erythropoietin) leads to a decrease in ERK, AKT and P70S6K phosphorylation of in lentivirus HCK silenced K562 and U937 cell lines[2].iHCK-37 (3-9 μM) results in a decrease of p-HCK, p-ERK, p-AKT, p-70S6 in the cell line KG1a (AML/CD34+), in a dose-dependent manner[2]. | [storage]
Store at -20°C | [References]
[1]. Cristina Tintori, et al. Identification of Hck inhibitors as hits for the development of antileukemia and anti-HIV agents. ChemMedChem. 2013 Aug;8(8):1353-60. [2]. Fernanda Marconi Roversi, et al. Hematopoietic cell kinase (HCK) is a potential therapeutic target for dysplastic and leukemic cells due to integration of erythropoietin/PI3K pathway and regulation of erythropoiesis: HCK in erythropoietin/PI3K pathway. Biochim Biophys Acta Mol Basis Dis. 2017 Feb;1863(2):450-461. |
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