LY2874455

Name: LY2874455
Brand: MedChemExpress
SKU: HY-13304
Rating: 5.0 (3 reviews)

Cat. No.: HY-13304 Purity: 98.03%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

LY2874455 Chemical Structure

CAS No. : 1254473-64-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 132	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 132	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE LY2874455

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View All Isoforms

FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target^[1]

FGFR1

2.8 nM (IC₅₀)

FGFR2

2.6 nM (IC₅₀)

FGFR3

6.4 nM (IC₅₀)

FGFR4

6 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.001 μM Compound: 5; LY2874455	Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing wild-type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	340.6 nM Compound: LY2874455	Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells expressing TEL-FGFR4 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
Hep 3B2	IC₅₀	0.001 μM Compound: 5; LY2874455	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
Hep 3B2	IC₅₀	260.8 nM Compound: LY2874455	Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Hep3B cells expressing FGF19/FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35635004]
MDA-MB-453	IC₅₀	0.005 μM Compound: 5; LY2874455	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
NCI-H1299	IC₅₀	0.059 μM Compound: 5; LY2874455	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
NCI-H1581	IC₅₀	< 0.5 nM Compound: 7	Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay Antiproliferative activity against FGFR1-amplified human NCI-H1581 cells after 72 hrs by CCK8/MTT assay	[PMID: 27348537]
NCI-H1581	IC₅₀	30.5 nM Compound: LY2874455	Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1581 cells expressing FGFR1 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
RT-112	IC₅₀	8.6 nM Compound: LY2874455	Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]
SNU-16	IC₅₀	2.2 nM Compound: LY2874455	Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antiproliferative activity against human SNU-16 cells expressing FGFR2 assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 35635004]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

444.31

Formula

C₂₁H₁₉Cl₂N₅O₂

CAS No.

1254473-64-7

Appearance

Solid

Color

Pink to gray

SMILES

ClC1=CN=CC(Cl)=C1[C@@H](C)OC2=CC=C(NN=C3/C=C/C4=CN(CCO)N=C4)C3=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (112.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2507 mL	11.2534 mL	22.5068 mL
5 mM	0.4501 mL	2.2507 mL	4.5014 mL
10 mM	0.2251 mL	1.1253 mL	2.2507 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.63 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.63 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.03%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (249 KB) LCMS (271 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Kinase Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2507 mL	11.2534 mL	22.5068 mL	56.2670 mL
	5 mM	0.4501 mL	2.2507 mL	4.5014 mL	11.2534 mL
	10 mM	0.2251 mL	1.1253 mL	2.2507 mL	5.6267 mL
	15 mM	0.1500 mL	0.7502 mL	1.5005 mL	3.7511 mL
	20 mM	0.1125 mL	0.5627 mL	1.1253 mL	2.8134 mL
	25 mM	0.0900 mL	0.4501 mL	0.9003 mL	2.2507 mL
	30 mM	0.0750 mL	0.3751 mL	0.7502 mL	1.8756 mL
	40 mM	0.0563 mL	0.2813 mL	0.5627 mL	1.4067 mL
	50 mM	0.0450 mL	0.2251 mL	0.4501 mL	1.1253 mL
	60 mM	0.0375 mL	0.1876 mL	0.3751 mL	0.9378 mL
	80 mM	0.0281 mL	0.1407 mL	0.2813 mL	0.7033 mL
	100 mM	0.0225 mL	0.1125 mL	0.2251 mL	0.5627 mL

LY2874455 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY28744551254473-64-7LY 2874455LY-2874455FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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LY2874455

Customer Review

LY2874455 Related Antibodies

3 Publications Citing Use of MCE LY2874455

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Biological Activity

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Purity & Documentation

References

Customer Review

LY2874455 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

LY2874455 Related Classifications

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