2640352-86-7
2640352-86-7 structure
- Name: FGFR2/3-IN-1
- Chemical Name: FGFR2/3-IN-1
- CAS Number: 2640352-86-7
- Molecular Formula: C23H22D3N7O3
- Molecular Weight: 450.51
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FGFR
- Create Date: 2023-02-14 17:25:34
- Modify Date: 2024-04-09 19:46:55
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FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
| Name | FGFR2/3-IN-1 |
|---|
| Description | FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1]. |
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| Related Catalog | |
| Target |
FGFR2:1 nM (IC50) FGFR3:0.5 nM (IC50) FGFR3 V555L:2.7 nM (IC50) FGFR3 V555M:6.1 nM (IC50) FGFR1:21 nM (IC50) FGFR4:145 nM (IC50) |
| In Vitro | FGFR2/3-IN-1 (compound 29) has a clean CYP profile (CYP3A4 IC50 >25 μM). FGFR2/3-IN-1 displays excellent potency (whole blood, IC50 = 177 nM) in a whole blood (WB) assay[1]. |
| In Vivo | FGFR2/3-IN-1 (compound 29) is advanced into rat pharmacokinetics studies. Clearance in the i.v. arm is low (hepatic blood flow (HBF) = 35%), with a moderate half-life (t1/2 = 1.7 h). In the p.o. dose, FGFR2/3-IN-1 demonstrates good exposure (AUC = 5108 nM·h) and high oral bioavailability (F% = 82)[2]. rat i.v. rat p.o. dose (mg/kg) 1.0 dose (mg/kg) 3.0 HBF% 35 Cmax (nM) 2303 Vdss (L/kg) 1.6 AUC (nM·h) 5108 T1/2 (h) 1.7 F% 82 |
| References |
| Molecular Formula | C23H22D3N7O3 |
|---|---|
| Molecular Weight | 450.51 |