FGFR2 degrader 1

Cat. No.: HY-162626: Data Sheet Handling Instructions
FAQs
Technical Support

FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC₅₀ of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase).

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

FGFR2 degrader 1 Chemical Structure

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

FGFR2

0.645 nM (DC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.627 μM Compound: 28e	Antiproliferative activity against human A2780 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]
AN3-CA	IC₅₀	4.626 nM Compound: 28e	Antiproliferative activity against human AN3-CA cells overexpressing FGFR2 measured after 72 hrs by MTT assay Antiproliferative activity against human AN3-CA cells overexpressing FGFR2 measured after 72 hrs by MTT assay	[PMID: 38908103]
BXPC-3	IC₅₀	0.997 μM Compound: 28e	Antiproliferative activity against human BXPC-3 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human BXPC-3 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]
BaF3	IC₅₀	0.2 nM Compound: 28e	Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR3 fusion protein incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR3 fusion protein incubated for 72 hrs by CCK-8 assay	[PMID: 38908103]
BaF3	IC₅₀	0.91 nM Compound: 28e	Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR2 fusion protein incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR2 fusion protein incubated for 72 hrs by CCK-8 assay	[PMID: 38908103]
BaF3	IC₅₀	27.5 nM Compound: 28e	Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR1 fusion protein incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR1 fusion protein incubated for 72 hrs by CCK-8 assay	[PMID: 38908103]
BaF3	IC₅₀	32.7 nM Compound: 28e	Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR4 fusion protein incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing wild type ETV6-FGFR4 fusion protein incubated for 72 hrs by CCK-8 assay	[PMID: 38908103]
HCT-116	IC₅₀	1.906 μM Compound: 28e	Antiproliferative activity against human HCT-116 cells expressing FGFR1/4 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells expressing FGFR1/4 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]
HEK-293T	IC₅₀	2.142 μM Compound: 28e	Cytotoxicity against HEK293T cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against HEK293T cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 38908103]
L02	IC₅₀	> 5 μM Compound: 28e	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 38908103]
MCF7	IC₅₀	2.983 μM Compound: 28e	Antiproliferative activity against human MCF7 cells expressing FGFR3 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells expressing FGFR3 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]
MDA-MB-231	IC₅₀	2.522 μM Compound: 28e	Antiproliferative activity against human MDA-MB-231 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells expressing FGFR1 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]
NCI-H1975	IC₅₀	2.239 μM Compound: 28e	Antiproliferative activity against EGFR-driven human NCI-H1975 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against EGFR-driven human NCI-H1975 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 38908103]
SNU-16	IC₅₀	0.207 nM Compound: 28e	Antiproliferative activity against FGFR2 amplified human SNU-16 cells measured after 72 hrs by MTT assay Antiproliferative activity against FGFR2 amplified human SNU-16 cells measured after 72 hrs by MTT assay	[PMID: 38908103]
SNU-449	IC₅₀	0.923 μM Compound: 28e	Antiproliferative activity against human SNU-449 cells expressing FGFR1/4 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SNU-449 cells expressing FGFR1/4 assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 38908103]

Molecular Weight

812.70

Formula

C₄₀H₃₉Cl₂N₉O₆

SMILES

O=C1N(C2C(NC(CC2)=O)=O)C(C3=CC(NCCCCCC(NCCN4N=CC(/C=C/C5=NNC6=CC=C(O[C@H](C)C7=C(Cl)C=NC=C7Cl)C=C56)=C4)=O)=CC=C31)=O

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

Handling Instructions (2659 KB)

References

[1]. Zuli Hu, et al. Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor. Eur J Med Chem. 2024 Sep 5:275:116612. [Content Brief]

FGFR2 degrader 1 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

FGFR2 degrader 1PROTACsFGFRFibroblast growth factor receptorAN3CA cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

FGFR2 degrader 1

FGFR2 degrader 1 Related Antibodies

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

FGFR2 degrader 1 Related Classifications

Molarity Calculator

Dilution Calculator