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Cat. No.: HY-170869

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PROTAC FGFR1 degrader-1

PROTAC FGFR1 degrader-1 is a PROTAC degrader targeting fibroblast growth factor receptor 1 (FGFR1), with a DC₅₀ of 39.78 nM and an IC₅₀ of 26.81 nM in KG1a cells. PROTAC FGFR1 degrader-1 selectively degrades FGFR1 via the ubiquitin-proteasome system, showing concentration- and time-dependent degradation in cancer cells. PROTAC FGFR1 degrader-1 can be used in studies related to leukemia and breast cancer.
(Pink: FGFR Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker (HY-W007587)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₄₆H₅₄N₈O₈
분자량:846.97

보관:

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

Data Sheet (278 KB)

PROTAC FGFR1 degrader-1 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Protocol (2)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

PROTAC FGFR1 degrader-1 is a PROTAC degrader targeting fibroblast growth factor receptor 1 (FGFR1), with a DC₅₀ of 39.78 nM and an IC₅₀ of 26.81 nM in KG1a cells. PROTAC FGFR1 degrader-1 selectively degrades FGFR1 via the ubiquitin-proteasome system, showing concentration- and time-dependent degradation in cancer cells. PROTAC FGFR1 degrader-1 can be used in studies related to leukemia and breast cancer^[1]. (Pink: FGFR Target protein ligand; Blue: Cereblon ligand (HY-10984); Black: linker (HY-W007587)).

IC₅₀ & Target

^[1]

FGFR1

39.78 nM (DC₅₀)

FGFR1

26.81 nM (IC₅₀)

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KG-1a	DC₅₀	39.78 nM	Half-maximal FGFR1 degradation in human KG1a leukemia cells assessed by western blot after 24 h incubation. Half-maximal FGFR1 degradation in human KG1a leukemia cells assessed by western blot after 24 h incubation.	39756204
KG-1a	IC₅₀	26.81 nM	Antiproliferative activity against human KG1a leukemia cells assessed by CCK-8 assay. Antiproliferative activity against human KG1a leukemia cells assessed by CCK-8 assay.	39756204
MCF7	IC₅₀	> 20 μM	Antiproliferative activity against human MCF-7 breast cancer cells assessed by CCK-8 assay, with no observed activity at concentrations up to 20 μM. Antiproliferative activity against human MCF-7 breast cancer cells assessed by CCK-8 assay, with no observed activity at concentrations up to 20 μM.	39756204

In Vitro

PROTAC FGFR1 degrader-1 (compound S2h) (1 μM; 72 h) degrades 71.7% of FGFR1 protein in MCF-7 cells^[1].
PROTAC FGFR1 degrader-1 (0.1-1 μM; 24 h) induces significant concentration-dependent degradation of FGFR1 protein in KG1a cells^[1].
PROTAC FGFR1 degrader-1 (0.1-10 μM; 72 h) selectively degrades FGFR1 (but not FGFR2, FGFR3 or FGFR4) in MCF-7 cells in a dose-dependent manner in vitro^[1].
PROTAC FGFR1 degrader-1 (7.8-500 nM; 24 h) induces concentration-dependent FGFR1 degradation in KG1a cells, with a DC₅₀ of 39.78 nM and a D_max of 78%^[1].
PROTAC FGFR1 degrader-1 (250 nM; 6-48 h) induces time-dependent degradation of FGFR1 in KG1a cells, with a significant reduction observed at 9 h and the maximum degradation achieved at 24 h^[1].
PROTAC FGFR1 degrader-1 potently inhibits the proliferation of KG1a cells with an IC₅₀ of 26.81 nM, but shows no activity against MCF-7 cells^[1].
PROTAC FGFR1 degrader-1 (250-1000 nM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in KG1a cells^[1].
PROTAC FGFR1 degrader-1 (62.5-500 nM; 72 h) induces dose-dependent apoptosis in KG1a cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MCF-7 human breast cancer cells
Concentration:

1 μM
Incubation Time:

72 h
Result:

Induced degradation of 71.7% of FGFR1 protein in MCF-7 cells.

Western Blot Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

0.1, 0.5, 1 μM
Incubation Time:

24 h
Result:

Induced significant concentration-dependent degradation of FGFR1 protein in KG1a cells.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MCF-7 human breast cancer cells
Concentration:

0.1,1, 10 μM
Incubation Time:

72 h
Result:

Selectively degraded FGFR1 in a dose-dependent manner.
No significant degradation of FGFR2, FGFR3, or FGFR4 was observed.

Western Blot Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

7.8, 15.6, 31.2, 62.5, 125, 250, 500 nM
Incubation Time:

24 h
Result:

Induced concentration-dependent FGFR1 degradation with no observed hook effect below 125 nM.
Achieved a half-maximal degradation concentration (DC₅₀) of 39.78 nM and a maximum degradation level (D_max) of 78%.

Western Blot Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

250 nM
Incubation Time:

6, 9, 12, 24, 48 h
Result:

Induced time-dependent FGFR1 degradation, with significant reduction observed at 9 h and maximum degradation achieved at 24 h.

Western Blot Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

250 nM (12 h incubation); 1 μM (72 h incubation)
Incubation Time:

12, 72 h
Result:

Pretreatment with MG132 completely blocked S2h-induced FGFR1 degradation.
Pretreatment with AZD4547 or pomalidomide notably inhibited degradation.
The negative control S2h-NEG showed significantly decreased FGFR1 degradation activity compared to S2h.

Cell Cycle Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

250, 500, 1000 nM
Incubation Time:

24 h
Result:

Induced weak G0/G1 phase cell cycle arrest at 250 nM, with significantly enhanced arrest at higher concentrations.

Apoptosis Analysis^[1]

View Protocol

Cell Line:

KG1a human leukemia cells
Concentration:

62.5, 125, 500 nM
Incubation Time:

72 h
Result:

Induced significant dose-dependent apoptosis of KG1a cells.
26.31% of cells underwent apoptosis at 500 nM, which was higher than the 15.8% apoptosis induced by 500 nM AZD4547.

Chemical Information

분자량 846.97
화학식 C₄₆H₅₄N₈O₈
SMILES

O=C(NC1=NNC(CCC2=CC(OC)=CC(OC)=C2)=C1)C3=CC=C(N4CCN(CCCCCCCCC(NC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3
선적

Room temperature in continental US; may vary elsewhere.
보관

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

Protocol

All Cell Biology Animals and Diseases

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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]. Wang YW, et al. Design, synthesis, and biological evaluation of novel FGFR1 PROTACs. Bioorganic chemistry. 2025 Feb;155:108109. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

견적 받기 해외재고보유

Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocol
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

PROTAC FGFR1 degrader-1

All PROTACs Isoforms

Biological Activity

제품 설명

IC50 & Target

Cellular Effect

In Vitro

Chemical Information

Protocol

순도&문서

References

Calculators

Help & FAQs