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PDGFR&FGFR

LY2874455 (1254473-64-7)

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.

Not Intended for Therapeutic Use. For research use only.

CAS: 1254473-64-7 Category

LY2874455 (1254473-64-7) Description:

LY2874455 is a novel and potent FGF/FGFR Inhibitor. It exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines and shows an excellent broad spectrum of antitumor activity in several tumor xenograft models representing the major FGF/FGFR relevant tumor histologies including lung, gastric, and bladder cancers and multiple myeloma, and with a well-defined pharmacokinetic/pharmacodynamic relationship.

LY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth.

LY2874455 (1254473-64-7) Specifications:

Product Name LY2874455
Synonym LY2874455; LY 2874455; LY-2874455.
Chemical Name (R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol.
Purity ≥98% (HPLC)
CAS Number 1254473-64-7
Molecular Formula C21H19Cl2N5O2
Molecular Weight 444.316 g/mol
Monoisotopic Mass 443.092 g/mol
MDL number MFCD22124884
InChIKey GKJCVYLDJWTWQU-CXLRFSCWSA-N
InChi Code 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
SMILES C[[email protected]](C1=C(Cl)C=NC=C1Cl)OC2=CC3=C(NN=C3/C=C/C4=CN(CCO)N=C4)C=C2
Form Powder
Color N/A
Solubility  DMSO 88 mg/mL (198.06 mM)

Water Insoluble

Alcohol 88 mg/mL (198.06 mM)

Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application a pan-FGFR inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai  Y, Huss K, Peng SB, McCann DJ. 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. 2011 Nov;10(11):2200-10. Epub 2011 Sep 7. PubMed PMID: 21900693.

[2]. LY2874455 potently inhibits FGFR gatekeeper mutants and overcomes mutation-based resistance. Wu D, Guo M, Min X, Dai S, Li M, Tan S, Li G, Chen X, Ma Y, Li J, Jiang L, Qu L, Zhou Z, Chen Z, Chen L, Xu G, Chen Y. Chem Commun (Camb). 2018 Oct 23;54(85):12089-12092. doi: 10.1039/c8cc07546h. PMID: 30298149

[3]. A Phase 1 Study of LY2874455, an Oral Selective pan-FGFR Inhibitor, in Patients with Advanced Cancer. Michael M, Bang YJ, Park YS, Kang YK, Kim TM, Hamid O, Thornton D, Tate SC, Raddad E, Tie J. Target Oncol. 2017 Aug;12(4):463-474. doi: 10.1007/s11523-017-0502-9. PMID: 28589492

[4]. Crystal Structure of the FGFR4/LY2874455 Complex Reveals Insights into the Pan-FGFR Selectivity of LY2874455. Wu D, Guo M, Philips MA, Qu L, Jiang L, Li J, Chen X, Chen Z, Chen L, Chen Y. PLoS One. 2016 Sep 12;11(9):e0162491. doi: 10.1371/journal.pone.0162491. eCollection 2016. PMID: 27618313

[5]. Acquired resistance to LY2874455 in FGFR2-amplified gastric cancer through an emergence of novel FGFR2-ACSL5 fusion. Kim SY, Ahn T, Bang H, Ham JS, Kim J, Kim ST, Jang J, Shim M, Kang SY, Park SH, Min BH, Lee H, Kang WK, Kim KM, Park W, Lee J. Oncotarget. 2017 Feb 28;8(9):15014-15022. doi: 10.18632/oncotarget.14788. PMID: 28122360

1 review for LY2874455 (1254473-64-7)

  1. Cofttek

    Never had such good experience before,The LY2874455 (1254473-64-7) is high purity,also customer service is pretty nice !gotta try!!

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