LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM.

Product information

CAS Number: 1088715-84-7

Molecular Weight: 1189.45

Formula: C62H88N14O10

Chemical Name: (2S)-2-{[(2S,5R,8S,11R,14S,20R)-2-benzyl-11-(3-carbamimidamidopropyl)-5-[(4-hydroxyphenyl)methyl]-14-[(naphthalen-2-yl)methyl]-3,6,9,12,15,18,23-heptaoxo-8-{4-[(propan-2-yl)amino]butyl}-1,4,7,10,13,16,19-heptaazacyclotricosan-20-yl]formamido}-6-[(propan-2-yl)amino]hexanamide

Smiles: CC(C)NCCCC[C@@H]1NC(=O)[C@@H](CC2C=CC(O)=CC=2)NC(=O)[C@H](CC2C=CC=CC=2)NC(=O)CC[C@@H](NC(=O)CNC(=O)[C@H](CC2=CC3=CC=CC=C3C=C2)NC(=O)[C@@H](CCCNC(N)=N)NC1=O)C(=O)N[C@@H](CCCCNC(C)C)C(N)=O

InChiKey: IJHWVENTEFSNBC-OFPUNPKKSA-N

InChi: InChI=1S/C62H88N14O10/c1-38(2)66-30-12-10-19-46(55(63)80)72-59(84)49-28-29-53(78)71-51(34-40-15-6-5-7-16-40)60(85)76-52(35-41-23-26-45(77)27-24-41)61(86)74-47(20-11-13-31-67-39(3)4)57(82)73-48(21-14-32-68-62(64)65)58(83)75-50(56(81)69-37-54(79)70-49)36-42-22-25-43-17-8-9-18-44(43)33-42/h5-9,15-18,22-27,33,38-39,46-52,66-67,77H,10-14,19-21,28-32,34-37H2,1-4H3,(H2,63,80)(H,69,81)(H,70,79)(H,71,78)(H,72,84)(H,73,82)(H,74,86)(H,75,83)(H,76,85)(H4,64,65,68)/t46-,47-,48+,49+,50-,51-,52+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 125 mg/mL (105.09 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.

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. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.

Products are for research use only. Not for human use.