LY2510924

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr HY-12488-50mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Description
LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. IC50 & Target: IC50: 0.079 nM (SDF-1 binding to CXCR4)[1] In Vitro: LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2]. In Vivo: LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity[1]. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells[2].
CAS No.
1088715-84-7
Purity
>98%
MW
1189, 45
Formula
C62H88N14O10
Solubility
DMSO: >=125 mg/mL
Clinical Phase
Phase 2
Signalling Pathway
GPCR/G Protein; Immunology/Inflammation
Target
CXCR; CXCR

Sicherheitsdatenblatt

HY-12488-50mg.pdf

Menge: 50mg
Lieferbar: In stock
Listenpreis: 2.275,36 €
Rabatt: -10,0%
Preis: 2.047,82 €
Sie sparen: 227,54 €
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