WH-4-023 - CAS 837422-57-8
Catalog number: 837422-57-8
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C32H36N6O4
Molecular Weight:
568.67
COA:
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Targets:
Src
Description:
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively. The lymphocyte-specific kinase (Lck) is a cytoplasmic tyrosine kinase of the Src family expressed in T cells and NK cells.
Purity:
0.98
Appearance:
Solid powder
Synonyms:
WH-4-023; WH4-023; WH 4-023; WH-4023; WH 4023; WH4023;
MSDS:
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InChIKey:
NBTNHSGBRGTFJS-UHFFFAOYSA-N
InChI:
InChI=1S/C32H36N6O4/c1-22-7-6-8-23(2)30(22)42-32(39)38(27-14-13-26(40-4)21-28(27)41-5)29-15-16-33-31(35-29)34-24-9-11-25(12-10-24)37-19-17-36(3)18-20-37/h6-16,21H,17-20H2,1-5H3,(H,33,34,35)
Canonical SMILES:
CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
Current Developer:
Amgen Inc
1.Glucocorticoid resistance is reverted by LCK inhibition in pediatric T-cell acute lymphoblastic leukemia.
Serafin V;Capuzzo G;Milani G;Minuzzo SA;Pinazza M;Bortolozzi R;Bresolin S;Porcù E;Frasson C;Indraccolo S;Basso G;Accordi B Blood. 2017 Dec 21;130(25):2750-2761. doi: 10.1182/blood-2017-05-784603. Epub 2017 Nov 3.
Pediatric T-acute lymphoblastic leukemia (T-ALL) patients often display resistance to glucocorticoid (GC) treatment. These patients, classified as prednisone poor responders (PPR), have poorer outcome than do the other pediatric T-ALL patients receiving a high-risk adapted therapy. Because glucocorticoids are administered to ALL patients during all the different phases of therapy, GC resistance represents an important challenge to improving the outcome for these patients. Mechanisms underlying resistance are not yet fully unraveled; thus our research focused on the identification of deregulated signaling pathways to point out new targeted approaches. We first identified, by reverse-phase protein arrays, the lymphocyte cell-specific protein-tyrosine kinase (LCK) as aberrantly activated in PPR patients. We showed that LCK inhibitors, such as dasatinib, bosutinib, nintedanib, and WH-4-023, are able to induce cell death in GC-resistant T-ALL cells, and remarkably, cotreatment with dexamethasone is able to reverse GC resistance, even at therapeutic drug concentrations. This was confirmed by specific ;LCK; gene silencing and ex vivo combined treatment of cells from PPR patient-derived xenografts.
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CAS 837422-57-8 WH-4-023

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