2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. Cytochrome P450 FGFR
  4. FGFR2/3-IN-3

FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to treat bone development disorder-related diseases such as achondroplasia (ACH).

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FGFR2/3-IN-3 Chemical Structure

FGFR2/3-IN-3 Chemical Structure

CAS No. : 3069945-78-1

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FGFR2/3-IN-3 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to treat bone development disorder-related diseases such as achondroplasia (ACH)[1].

IC50 & Target

CYP2C9

3.9 μM (IC50)

CYP2D6

5.0 μM (IC50)

CYP3A4M

7.2 μM (IC50)

FGFR3

3.9 nM (IC50)

FGFR2

2.7 nM (IC50)

In Vitro

FGFR2/3-IN-3 (compound 23) exhibits potent inhibitory activity against both wild-type (IC50 = 3.2 nM) and V555M mutant (IC50 = 0.5 nM) FGFR3, as well as TEL-FGFR1 (IC50 = 29.4 nM) and TEL-FGFR4 (IC50 = 29 nM)[1].

FGFR2/3-IN-3 exhibits inhibiting activity on the common FGFR3G380R (IC50 = 7.0 nM), FGFR3WT (IC50 = 3.9 nM), FGFR3V555L (IC50 = 1.7 nM), FGFR3L608V (IC50 = 10.0 nM), mutation in ACH in TEL-FGFR3 Mutant Ba/F3 Cell Lines[1].

FGFR2/3-IN-3 inhibits the growth of RT-112/84 cell (IC50 = 1.3 nM) in FGFR3-driven tumor cells[1].

FGFR2/3-IN-3 demonstrates slightly stronger inhibitory activity against the CYP subtypes 2C9 (IC50 = 3.9 μM) and 2D6 (IC50 = 5.0 μM) compared to the 3A4 subtype[1].

FGFR2/3-IN-3 (Compound 23) (0.2 μM, 1 μM) rescues FGF-induced growth retardation in an ex vivo fetal mouse femur culture model[1].

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

FGFR2/3-IN-3 Related Antibodies
In Vivo

FGFR2/3-IN-3 (0.5 mg/kg, 2 mg/kg, s.c., 14 days) enhances overall body growth promotion as well as the growth increase for tail, tibia, and femur in the Fgfr3Y367C/+ mouse model of ACH[1].

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

Animal Model: Fgfr3Y367C/+ mouse model of ACH[1]
Dosage: 0.5 mg/kg, 2 mg/kg
Administration: s.c., 14 days
Result: Enhances overall body growth promotion as well as the growth increase for tail, tibia, and femur.
Molecular Weight

569.46

Formula

C28H27Cl2FN6O2
CAS No.
SMILES

CC(C)(CN1N=C(C(C2=NC=C(C=C2F)C3=NNC4=C3C=C(C(C)=C4)O[C@H](C)C5=C(C=NC=C5Cl)Cl)=C1)C)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
References
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FGFR2/3-IN-3 Related Classifications

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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:

FGFR2/3-IN-33069945-78-1Cytochrome P450FGFRCYPsFibroblast growth factor receptorInhibitorhERG cellsBa/F3 Cell LinesRT-112/84 cellFgfr3Y367C/+ mouse model of ACHEx vivo fetal mouse femur culture modelinhibitorinhibit

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