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1088715-84-7 (LY2510924)

1

Identification

LY2510924 LY2510924
Name LY2510924
Formula C62H88N14O10
MW 1189.45
CAS No. 1088715-84-7
EINECS
Smiles O=C(NCC(N[[email protected]](CCC(N[[email protected]]1CC2=CC=CC=C2)=O)C(N[[email protected]](C(N)=O)CCCCNC(C)C)=O)=O)[[email protected]@H](NC([[email protected]@](NC([[email protected]@H](NC([[email protected]](NC1=O)CC3=CC=C(O)C=C3)=O)CCCCNC(C)C)=O)([H])CCCNC(N)=N)=O)CC4=CC(C=CC=C5)=C5C=C4
Synonyms (2S,5R,8S,11R,14S,20R)-N-((S)-1-amino-6-(isopropylamino)-1-oxohexan-2-yl)-2-benzyl-11-(3-guanidinopropyl)-5-(4-hydroxybenzyl)-8-(4-(isopropylamino)butyl)-14-(naphthalen-2-ylmethyl)-3,6,9,12,15,18,23-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosane-20-carboxamide
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
2

Introduction

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

Background Information

LY-2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4). It has potential antineoplastic activity. It binds to the chemokine receptor CXCR4, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor a ......by BOC Sciences
LY2510924 is a potent and selective CXCR4 antagonist; blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. ......by MedChemexpress Co., Ltd.
LY2510924 is an inhibitor of CXC chemokine receptor 4 (CXCR4), with potential antineoplastic activity. Upon subcutaneous administration, CXCR4 inhibitor LY2510924 binds to the chemokine receptor CXCR4, thereby preventing CXCR4 binding to its ligand, stromal derived factor-1 (SDF-1), and subsequent receptor activation. This may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types. ......by MedKoo Biosciences, Inc.
LY-2510924 (LY2510924) is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity; inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling; exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells; shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.Kidney CancerPhase 2 Clinical ......by ProbeChem
LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L. ......by Selleck Chemicals LLC
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000123352

Storage condition

Solubility

DMSO: ≥125 mg/mL by CHEMSCENE, LLC
DMSO: ≥125 mg/mL by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LY2510924 M.D. Anderson Cancer Center|Eli Lilly and Company|High Impact Clinical Research Support Program Leukemia 2016/5/1 Phase 1
LY2510924 Eli Lilly and Company|AstraZeneca Solid Tumor 2016/9/1 Phase 1
LY2510924 Eli Lilly and Company Metastatic Clear Cell Renal Cell Carcinoma 2011/8/1 Phase 2
LY2510924 Eli Lilly and Company Extensive Stage Small Cell Lung Carcinoma 2011/9/1 Phase 2
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Safety Data of LY2510924

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 1mg/USD120();5mg/USD420() USA
MedChemexpress Co., Ltd. 1mg/USD120();5mg/USD420() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 1mg/USD120();5mg/USD420() China
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Related Products

Other Forms of 1088715-84-7

Name CAS No Formula MW

Recommended Compounds in CXCR

Name CAS No Formula MW
AMD 3465 185991-24-6 C24H38N6 410.6
AMD 3465 185991-24-6 C24H38N6 410.5987
AZD8797 911715-90-7 C19H25N5OS2 403.5647
Baohuoside I 113558-15-9 C27H30O10 514.52
AMD-070 hydrochloride C21H30Cl3N5 458.86
WZ811 55778-02-4 C18H18N4 290.36
SRT3109 1204707-71-0 C18H23F2N5O4S2 475.53
UNBS5162 956590-23-1 C17H18N4O3 326.3498
NBI-74330 855527-92-3 C32H27F4N5O3 605.58
AMG 487 473719-41-4 C32H28F3N5O4 603.59
Reparixin (L-lysine salt) 266359-93-7 C20H35N3O5S 429.57
Reparixin 266359-83-5 C14H21NO3S 283.39
SCH 546738 906805-42-3 C23H31Cl2N7O 492.44
SCH 563705 473728-58-4 C23H27N3O5 425.48
SCH 527123 473727-83-2 C21H23N3O5 397.42
Plerixafor 110078-46-1 C28H54N8 502.78
AMD-070 558447-26-0 C21H27N5 349.47
Plerixafor (octahydrochloride) 155148-31-5 C28H62Cl8N8 794.47
SRT3190 1204707-73-2 C18H23F2N5O4S2 475.53
Nicotinamide N-oxide 1986-81-8 C6H6N2O2 138.12404

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Nordihydroguaiaretic acid 500-38-9 C18H22O4 302.36
Pazopanib (Hydrochloride) 635702-64-6 C21H24ClN7O2S 473.98
RX-3117 865838-26-2 C10H12FN3O4 257.22
OSU-03012 742112-33-0 C26H19F3N4O 460.45
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
LY2603618 911222-45-2 C18H22BrN5O3 436.3
AT13387 912999-49-6 C24H31N3O3 409.52
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
Delanzomib 847499-27-8 C21H28BN3O5 413.28
SU14813 (maleate) 849643-15-8 C27H31FN4O8 558.56
AT7519 844442-38-2 C16H17Cl2N5O2 382.24
5-Azacytidine 320-67-2 C8H12N4O5 244.2
Plinabulin 714272-27-2 C19H20N4O2 336.39
BMS-599626 714971-09-2 C27H27FN8O3 530.55
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Route of Synthesis

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References

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More Information

LY2510924

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