LY2874455

Modify Date: 2026-07-03 14:58:37

LY2874455 Structure
LY2874455 structure
 Common Name LY2874455
CAS Number 1254473-64-7 Molecular Weight 444.314
Density 1.4±0.1 g/cm3 Boiling Point 672.6±55.0 °C at 760 mmHg
Molecular Formula C21H19Cl2N5O2 Melting Point N/A
MSDS N/A Flash Point 360.5±31.5 °C

 Use of LY2874455


LY2874455 is a pan-FGFR inhibitor with IC50s of 2.8, 2.6, 6.4, 6 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively.

 Names

This table lists Chinese names, IUPAC names and various aliases of this chemical substance.

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

 LY2874455 Biological Activity

This table contains bioactivity, target information and biological‑assay experimental data of this compound.

Description LY2874455 is a pan-FGFR inhibitor with IC50s of 2.8, 2.6, 6.4, 6 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively.
Related Catalog
Target

FGFR1:2.8 nM (IC50)

FGFR2:2.6 nM (IC50)

FGFR3:6.4 nM (IC50)

FGFR4:6 nM (IC50)

In Vitro LY2874455 potently inhibits the Erk phosphorylation induced by FGF2 and FGF9 in both cell lines in a dose-dependent manner, with average IC50 values of 0.3 to 0.8 nM. LY2874455 indeed inhibits FGFR2 phosphorylation in SNU-16 and KATO-III cells, with estimated IC50 values of 0.8 and 1.5 nM, respectively. In addition, LY2874455 inhibits the phosphorylation of FRS2, an immediate downstream target of FGFR in these cell lines, again with a similar potency of 0.8 to 1.5 nM. Together, these results suggest that LY2874455 inhibits FGFR in the cell. The relative IC50 values of LY2874455 for KMS-11, OPM-2, L-363, and U266 cells are determined to be 0.57, 1.0, 60.4, and 290.7 nM, respectively[1].
In Vivo LY2874455 exhibits a rapid, robust, dose-dependent inhibition of tumor growth in all 4 models tested. Importantly, this molecule causes a significant regression of tumor growth in the RT-112, SNU-16, and OPM-2 tumor models, especially when dosed at 3 mg/kg twice a day. Also, LY2874455 exhibits an excellent pharmacokinetic/pharmacodynamic relationship as shown by its dose-dependent inhibition of the tumor growth at TED50 and TED90 (1 and 3 mg/kg, respectively). When tested in the RT-112 tumor xenograft model on an intermittent dosing schedule (twice a day 1 week on and 1 week off or twice a day 2 days on and 2 days off), LY2874455 is also efficacious. When rats are dosed with LY2874455 at 1 and 3 mg/kg, which is 2.6- and 7.7-fold over the TED50 (0.39 mg/kg) obtained in the rat heart IVTI assay, respectively, there are no significant changes observed in blood pressure. However, when rats are dosed with LY2874455 at 10 mg/kg, which is 25.6-fold over the TED50, there are significant increases observed in arterial pressures[1].
Kinase Assay Reaction mixtures contained 8 mM Tris-HCl (pH 7.5), 10 mM HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% DMSO, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20-50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader[1].
Cell Assay The different multiple myeloma cancer cell lines KMS-11 and OPM-2 cells, L-363, and U266 cells are used. Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37°C for 3 days. The cells are stained at 37°C for 4 hours and then solubilized at 37°C for 1 hour. Finally, the plate is read at 570 nm using a plate reader[1].
Animal Admin Mice[1] RT-112, OPM-2 (DSMZ), SNU-16, and NCI-H460 cells (RT-112: 2×106 per animal; OPM-2: 107 per animal; SNU-16: 106 per animal; and NCI-H460: 3×106 per animal) are mixed with Matrigel (1:1) and implanted subcutaneously into the rear flank of the mice (female, CD-1 nu/nu for RT-112, OPM-2, and NCI-H460 cells and female, severe combined immunodeficient for SNU-16 cells). The implanted tumor cells grow as solid tumors. To test the efficacy of LY2874455 in these models, the animals are orally dosed with approximately 1 mg/kg (TED50) or 3 mg/kg (TED90) of LY2874455 in 10% Acacia once (every day) or twice a day after tumors reach approximately 150 mm3. The tumor volume and body weight are measured twice a week. Rats[1] Four male rats per group are dosed with vehicle (1% hydroxyethylcellulose, 0.25% polysorbate 80, and 0.05% Dow Corning antifoam 1510-US in purified water) on day 1 and LY2874455 (1, 3, and 10 mg/kg) on day 0. On day 1, at least 120 minutes of control data are collected following vehicle administration. On day 0, data are collected for approximately 20 hours beginning after the last animal is dosed.
References

[1]. Zhao G, 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.

 Chemical & Physical Properties

This table shows physicochemical parameters including melting point, boiling point, density, solubility and optical rotation. Missing data is marked as N/A.

Density 1.4±0.1 g/cm3
Boiling Point 672.6±55.0 °C at 760 mmHg
Molecular Formula C21H19Cl2N5O2
Molecular Weight 444.314
Flash Point 360.5±31.5 °C
Exact Mass 443.091583
PSA 88.85000
LogP 3.88
Vapour Pressure 0.0±2.2 mmHg at 25°C
Index of Refraction 1.683
InChIKey GKJCVYLDJWTWQU-CXLRFSCWSA-N
SMILES CC(Oc1ccc2[nH]nc(C=Cc3cnn(CCO)c3)c2c1)c1c(Cl)cncc1Cl

 Safety Information

This table covers safety warnings, protective measures, incompatible substances and disposal guidelines for this compound.

Hazard Codes Xi

 Synthetic Route

This table presents publicly reported synthetic routes, reaction conditions, reactants and product information of the compound.

5-((R)-1-(3,5-Dichloropyridin-4-yl)ethoxy)-1-(tetrahydro-2H-pyran-2-yl)-3-((E)-2-(1-(2-(tetrahydro-2H-pyran-2-yloxy)ethyl)-1H-pyrazol-4-yl)vinyl)-1H-indazole structure

5-((R)-1-(3,5-D...

CAS#:1254473-82-9

~41%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: ELI LILLY AND COMPANY Patent: US2012/83511 A1, 2012 ; Location in patent: Page/Page column 3 ;
1H-Indazol-5-ol structure

1H-Indazol-5-ol

CAS#:15579-15-4

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
4-iodo-1-[2-(oxan-2-yloxy)ethyl]pyrazole structure

4-iodo-1-[2-(ox...

CAS#:879487-88-4

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
5-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-1H-Indazole structure

5-[[(1,1-dimeth...

CAS#:1254473-74-9

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
5-((tert-Butyldimethylsilyl)oxy)-3-iodo-1H-indazole structure

5-((tert-Butyld...

CAS#:1254473-76-1

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
5-(tert-butyldimethylsilyloxy)-3-iodo-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole structure

5-(tert-butyldi...

CAS#:1254473-78-3

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
3,5-Dichloropyridine structure

3,5-Dichloropyridine

CAS#:2457-47-8

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
4-PyridineMethanol, 3,5-dichloro-α-Methyl structure

4-PyridineMetha...

CAS#:1254473-66-9

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;
(S)-1-(3,5-dichloropyridin-4-yl)ethanol structure

(S)-1-(3,5-dich...

CAS#:1370347-50-4

~%

LY2874455 Structure

LY2874455

CAS#:1254473-64-7

Learn More
Literature: US2012/83511 A1, ;

 Precursor & DownStream

This table lists upstream starting materials and downstream derivative products related to this chemical.

Precursor  4

DownStream  0

 LY2874455Bioassay

View more

This table contains target information, in‑vitro & in‑vivo assay data for this compound.

Name: Antiproliferative activity against FGFR2 amplified human KATO III cells assessed as r...
Source: ChEMBL
Target: KATO III stomach cancer cell line
External Id: CHEMBL5581412
Name: Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
Source: NCGC
Target: N/A
External Id: TRND-SARS-CoV-2-cytotox-48hr
Name: Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incub...
Source: ChEMBL
Target: Fibroblast growth factor receptor 4
External Id: CHEMBL4723294
Name: Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation...
Source: ChEMBL
Target: Fibroblast growth factor receptor 4
External Id: CHEMBL4723295
Name: Hepatic extraction ratio in rat liver microsomes preincubated for 3 mins followed by ...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4723292
Name: Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
Source: NCGC
External Id: TRND-SARS-CoV-2-PP
Name: Inhibition of FGFR1 (unknown origin)
Source: ChEMBL
Target: Fibroblast growth factor receptor 1
External Id: CHEMBL5623895
Name: Inhibition of FGFR4 (445 to 753 residues) (unknown origin) expressed in Escherichia c...
Source: ChEMBL
Target: Fibroblast growth factor receptor 4
External Id: CHEMBL5623896
Name: Antiproliferative activity against human Huh-7 cells measured after 24 to 48 hrs by M...
Source: ChEMBL
Target: Huh-7
External Id: CHEMBL5623897
Name: Inhibition of FGFR2 (unknown origin)
Source: ChEMBL
Target: Fibroblast growth factor receptor 2
External Id: CHEMBL5623899
Total 77, Current Page 1 of 8
1
2
3
4
5

 Synonyms

This table collects all English aliases, systematic names and CAS‑related synonyms of the compound.

(R)-(E)-2-(4-(2-(5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)vinyl)-1H-pyrazol-1-yl)ethanol
2-{4-[(E)-2-{5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl}vinyl]-1H-pyrazol-1-yl}ethanol
CS-0907
4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol
QCR-90
LY2874455
LY-2874455

 LY2874455 | FAQ

This section contains frequently‑asked‑questions about this compound, including basic parameters, properties, storage conditions and corresponding answers.

Q: What is the polar surface area (PSA) of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: Polar surface area (PSA) of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 88.85000.
Q: What is the molecular formula of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: Molecular formula of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is C21H19Cl2N5O2.
Q: What are the upstream materials of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: Related upstream materials(CAS) of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol: 15579-15-4;879487-88-4;2457-47-8;1370347-50-4.
Q: What is the InChIKey of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: InChIKey of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is GKJCVYLDJWTWQU-CXLRFSCWSA-N.
Q: What is the boiling point of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: Boiling point of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 672.6±55.0 °C at 760 mmHg.
Q: What English synonyms does 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol have?
A: English synonyms of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]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, 2-{4-[(E)-2-{5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl}vinyl]-1H-pyrazol-1-yl}ethanol, CS-0907, 4-[(1E)-2-[5-[(1R)-1-(3,5-Dichloro-4-pyridinyl)ethoxy]-1H-indazol-3-yl]ethenyl]-1H-pyrazole-1-ethanol, QCR-90, LY2874455, LY-2874455.
Q: What is the CAS number of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: CAS number of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 1254473-64-7.
Q: What is the LogP of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: LogP of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 3.88.
Q: What is the molecular weight of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: Molecular weight of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 444.314.
Q: What is the English name of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol?
A: The English name of 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol is 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol.

 LY2874455factory

This table lists manufacturers and suppliers of this compound, including vendor names and product supply reference information.

Shanghai Nianxing Industrial Co., Ltd
Dayang Chem (Hangzhou) Co., Ltd.
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.
Top Suppliers:I want be here

Get all suppliers and price by the below link:

LY2874455 suppliers

Price: $172/10mM*1mLinDMSO

Reference only. check more LY2874455 price

Related Compounds: More...
Propyl 2,3,3,3-tetrafluoro-2-[1,1,2,3,3,3-hexafluoro-2-(heptafluoropropoxy)propoxy]propanoate
145510-87-8
Propan-2-yl 2,3,3,3-tetrafluoro-2-[1,1,2,3,3,3-hexafluoro-2-(heptafluoropropoxy)propoxy]propanoate
145510-88-9
4-(4-Butyl-2,3,5,6-tetrafluorophenyl)aniline
131894-92-3
2-Hydroxy-3-(3,4,5-trimethoxyphenyl)propanoic acid
76774-04-4
coenzyme II
165676-60-8
Methyl (2R)-1-(2-{[(benzyloxy)carbonyl]amino}acetyl)pyrrolidine-2-carboxylate
2365390-46-9
(3S)-1,3-dimethyl-3,4-dihydro-1,4-benzodiazepine-2,5-dione
104873-99-6
(2R)-2-(dimethylamino)butanedioic acid
77270-86-1
8-Bromo-9H-pyrido[3,4-b]indole
144434-77-5
2,4-Dichloro-1-(4-chlorobutoxy)benzene
23468-04-4
Chemsrc provides LY2874455(CAS#:1254473-64-7) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of LY2874455 are included as well.>> amp version: LY2874455

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2026 ChemSrc All Rights Reserved