LY 2874455

Description

Product Name: LY 2874455
CAS No.: 1254473-64-7
Chemical Name: LY 2874455
Synonyms: CS-650;EOS-62114;LY 2874455;LY2874455/LY-2874455;LY 2874455 USP/EP/BP;LY 2874455; LY-2874455;LY2874455;(R,E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)-ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl);(E)-2-(4-(2-(5-(1-(3,5-DICHLOROPYRIDIN-4-YL)ETHOXY)-1H-INDAZOL-3-YL)VINYL)-1H-PYRAZOL-1-YL)ETHANOL;(R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol;4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol
CBNumber: CB12616026
Molecular Formula: C21H19Cl2N5O2
Formula Weight: 444.31
MOL File: 1254473-64-7.mol

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LY 2874455 Property

Boiling point:: 672.6±55.0 °C(Predicted)
Density: 1.44
storage temp.: Store at -20°C
solubility: ≥44.4 mg/mL in DMSO; insoluble in H2O; ≥6.34 mg/mL in EtOH with gentle warming and ultrasonic
form: solid
pka: 12.93±0.40(Predicted)
color: Pink to gray
CAS DataBase Reference: 1254473-64-7

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 20843
Product name: LY2874455
Purity: ≥98%
Packaging: 1mg
Price: $74
Updated: 2024/03/01

Cayman Chemical

Product number: 20843
Product name: LY2874455
Purity: ≥98%
Packaging: 5mg
Price: $220
Updated: 2024/03/01

Cayman Chemical

Product number: 20843
Product name: LY2874455
Purity: ≥98%
Packaging: 10mg
Price: $330
Updated: 2024/03/01

Cayman Chemical

Product number: 20843
Product name: LY2874455
Purity: ≥98%
Packaging: 25mg
Price: $437
Updated: 2024/03/01

TRC

Product number: L486580
Product name: LY2874455
Packaging: 25mg
Price: $365
Updated: 2021/12/16

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LY 2874455 Chemical Properties,Usage,Production

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.

Uses

LY 2874455 is a pan-FGFR inhibitor which remain the focus of research for use in lung and bladder cancers.

Biological Activity

ly2874455 is a novel and potent fgfr inhibitor with ic50 value of 7 nm [1].fibroblast growth factor receptors (fgfrs) are receptors bind ligand of fgf family, which have a intracellular domain with tyrosine kinase activity. the binding of fgf triggers receptor dimerization and thus the activation of tyrosine kinase activity. activated tyrosine kinase phosphorylates various downstream factors to induce downstream signaling, including fgf substrate 2 (fgs2). this signaling pathway contributes to fgfr-mediated cell proliferation and migration, which are involved in tumor formation and progression.in huvecs cell line expressing fgfr1 and rt-112 cell line expressing fgfr3, ly2874455 treatment resulted in inhibition of fgf2 and fgf9 induced erk phosphorylation, which indicated the inhibitory activity of ly2874455 for fgfr1 and fgfr3 [1]. in snu-16 and kato-ш cell line, the inhibition of fgfr2 phosphorylation was also observed, which indicated a direct inhibition by ly2874455 [2]. additionally, when several multiple myeloma cancer cell lines were treated with lys2874455, the cell lines with chromosomal translocation that resulted in overexpression of fgfr3 were significantly more susceptible to the inhibition of ly2874455 [2]. it suggested fgfr was the specific target of ly2874455 inhibition.in rt-112, snu-16, opm-2 and nci-h460 xenograft tumor model, treatment of ly2874455 twice a day (1.5 mg/kg and 3 mg/kg) resulted in significant dose-dependent reduction of cellular level of phosphorylated fgfr, and also regression of tumor growth. it indicated the inhibitory activity of ly2874455 in vivo [2].

target

FGFR1

References

[1] zhao, g s et al. , a novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. molecular cancer therapeutics. 2011, 10(11): 2200-2210.

LY 2874455 Preparation Products And Raw materials

Raw materials

Preparation Products

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LY 2874455 Suppliers

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View Lastest Price from LY 2874455 manufacturers

Career Henan Chemical Co

Product: LY 2874455 1254473-64-7
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

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LY 2874455

(R,E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol

CS-650

LY 2874455; LY-2874455;LY2874455

4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol

LY2874455/LY-2874455

4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol LY2874455

(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

(R,E)-2-(4-(2-(5-(1-(3,5-Dichloropyridin-4-yl)-ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)

(E)-2-(4-(2-(5-(1-(3,5-DICHLOROPYRIDIN-4-YL)ETHOXY)-1H-INDAZOL-3-YL)VINYL)-1H-PYRAZOL-1-YL)ETHANOL

EOS-62114

1H-Pyrazole-1-ethanol, 4-[(1E)-2-[5-[(1R)-1-(3,5-dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-

LY 2874455 USP/EP/BP

2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol

1254473-64-7

C21H19Cl2N5O2

Inhibitors