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Cat. No.: HY-162626

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PROTAC FGFR2 degrader 2

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).
(Pink: FGFR2 ligand (HY-13304); Blue: Cereblon ligand (HY-W087383); Black: linker).

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

CAS No.: 3080487-43-7
Formula: C₄₀H₃₉Cl₂N₉O₆
Molecular Weight:812.70

Storage:

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

Data Sheet (266 KB)

PROTAC FGFR2 degrader 2 Chemical Structure

CAS No.: 3080487-43-7

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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)^[1]. (Pink: FGFR2 ligand (HY-13304); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC₅₀ & Target

FGFR2

0.645 nM (DC₅₀)

All PROTACs Isoforms :

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]
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]
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]
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]

Chemical Information

CAS No. 3080487-43-7
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (266 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]. 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]

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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.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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PROTAC FGFR2 degrader 2

All PROTACs Isoforms