country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-145836

Copy Link Print Information

FGFR4-IN-8

FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4^V550L, FGFR4^V550M and FGFR4^C552S with IC₅₀s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC₅₀ value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model.

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

CAS No.: 2765240-52-4
Formula: C₃₂H₃₄Cl₂FN₇O₃
Molecular Weight:654.56

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

FGFR4-IN-8 Chemical Structure

CAS No.: 2765240-52-4

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>1 μM Compound: 7v	Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	0.0035 μM Compound: 7v	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	4.7 nM Compound: 7v	Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
BaF3	IC₅₀	8.1 nM Compound: 7v	Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells expressing FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 35271262]
Hep 3B2	IC₅₀	0.029 μM Compound: 7v	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]
Huh-7	IC₅₀	72 nM Compound: 7v	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth incubated for 5 days by SRB assay	[PMID: 35271262]
MDA-MB-453	IC₅₀	0.034 μM Compound: 7v	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	2.97 μM Compound: 7v	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]

Chemical Information

CAS No. 2765240-52-4
Molecular Weight 654.56
Formula C₃₂H₃₄Cl₂FN₇O₃
SMILES

C[C@@H](OC1=CC=C(C2=C1)NN=C2NC3=C(C=C(C=C3F)N4CCC(CC4)N5CCOCC5)NC(C=C)=O)C6=C(C=NC=C6Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Min Shao, et al. Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4. J Med Chem. 2022 Mar 24;65(6):5113-5133. [Content Brief]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

Get Quote In-stock