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 study bone development disorder-related diseases such as achondroplasia (ACH).
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- CAS 番号: 3069945-78-1
- 分子式: C28H27Cl2FN6O2
- 分子量:569.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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) |
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 (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.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | CL | F |
|---|---|---|---|---|---|---|---|---|
| Mice | 0.5 mg/kg | s.c. | 2.3 h | 1.3 h | 49.2 ng/mL | 228 ng·h/mL | / | / |
| Mice | 1 mg/kg | s.c. | 2.0 h | 1.7 h | 100 ng/mL | 449 ng·h/mL | / | / |
| Mice | 2 mg/kg | s.c. | 2.8 h | 2.7 h | 171 ng/mL | 1127 ng·h/mL | / | / |
| Rat | 1 mg/kg | i.v. | / | / | / | 965 ng·h/mL | 18 mL/min/kg | / |
| Rat | 10 mg/kg | p.o. | / | 8.0 h | 517 ng/mL | 6909 ng·h/mL | / | 52 % |
| Rat | 2 mg/kg | p.o. | 4.3 h | 5.7 h | 27.9 ng/mL | 209 ng·h/mL | / | / |
| Rat | 20 mg/kg | p.o. | / | 8.0 h | 1273 ng/mL | 18373 ng·h/mL | / | 98.6 % |
| Rat | 5 mg/kg | p.o. | / | 6.7 h | 211 ng/mL | 2424 ng·h/mL | / | 52 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fgfr3Y367C/+ mouse model of ACH[1]
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Dosage:0.5 mg/kg, 2 mg/kg
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Administration:s.c., 14 days
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Result:Enhanced overall body growth promotion as well as the growth increase for tail, tibia, and femur.
化学情報
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CAS 番号 3069945-78-1
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分子量 569.46
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分子式 C28H27Cl2FN6O2
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FGFR2/3-IN-3 関連分類
HY-176547 関連分類
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