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LY2874455 - ≥99%, high purity , CAS No.1254473-64-7, Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fibroblast growth factor receptor 2;Inhibitor of fibroblast growth factor receptor 3;Inhibitor of fibroblast growth factor receptor 4;Inhibitor of kinase insert domain receptor

Moligand™
≥99%

CAS#: 1254473-64-7
Formula: C₂₁H₁₉Cl₂N₅O₂
Molecular Weight: 444.31
PubChem CID: 46944259

Item Number

L126507

Grouped product items
SKU	Size	Availability	Price
L126507-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$169.90
L126507-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$273.90
L126507-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$888.90

Potent FGF/FGFR inhibitor

View related series

fibroblast growth factor receptor 1 Inhibitor fibroblast growth factor receptor 2 Inhibitor fibroblast growth factor receptor 3 Inhibitor fibroblast growth factor receptor 4 Inhibitor kinase insert domain receptor Inhibitor

Basic Description

Synonyms	LY2874455\|1254473-64-7\|LY-2874455\|LY 2874455\|CHEMBL3828009\|E9M363811V\|(R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethan-1-ol\|1H-Pyrazole-1-ethanol, 4-((1E)-2-(5-((1R)-1-(3,5-dichloro-4-pyridinyl)ethoxy)-1H-
Specifications & Purity	≥99%
Storage Temp	Store at -20°C
Shipped In	Dry ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fibroblast growth factor receptor 2;Inhibitor of fibroblast growth factor receptor 3;Inhibitor of fibroblast growth factor receptor 4;Inhibitor of kinase insert domain receptor
Product Description	LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.

Associated Targets

FGFR1 Tclin Fibroblast growth factor receptor 1 5 Activities

Discover Target: FGFR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 3 Activities

Discover Target: FGFR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR4 Tclin Fibroblast growth factor receptor 4 5 Activities

Discover Target: FGFR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 3 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 2 Activities

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol
INCHI	InChI=1S/C21H19Cl2N5O2/c1-13(21-17(22)10-24-11-18(21)23)30-15-3-5-20-16(8-15)19(26-27-20)4-2-14-9-25-28(12-14)6-7-29/h2-5,8-13,29H,6-7H2,1H3,(H,26,27)/b4-2+/t13-/m1/s1
InChi Key	GKJCVYLDJWTWQU-CXLRFSCWSA-N
Canonical SMILES	CC(C1=C(C=NC=C1Cl)Cl)OC2=CC3=C(C=C2)NN=C3C=CC4=CN(N=C4)CCO
Isomeric SMILES	C[C@H](C1=C(C=NC=C1Cl)Cl)OC2=CC3=C(C=C2)NN=C3/C=C/C4=CN(N=C4)CCO
PubChem CID	46944259
Molecular Weight	444.31

PubChem CID

46944259

CAS Registry No.

1254473-64-7

RCSB PDB Ligand

6LF

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Lot Number	Certificate Type	Date	Item
J1521095	Certificate of Analysis	May 10, 2023	L126507

References

1. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K et al.. (2011) A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models.. Mol Cancer Ther, 10 (11): (2200-10). [PMID:21900693]
2. Molè MA et al.. (2021) A single cell characterisation of human embryogenesis identifies pluripotency transitions and putative anterior hypoblast centre.. Nat Commun, 12 (3679). [PMID:34140473]

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