FGFR-IN-8
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2640217-64-5
- Formule: C27H31Cl2N9O2
- Masse moléculaire:584.50
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
|
FGFR1 <0.5 nM (IC50) |
N549H-FGFR2 <0.5 nM (IC50) |
FGFR3 <0.5 nM (IC50) |
K650E-FGFR3 <0.5 nM (IC50) |
K650M-FGFR3 4.8 nM (IC50) |
FGFR4 7.30 nM (IC50) |
V555M-FGFR3 22.6 nM (IC50) |
V564F-FGFR2 189.1 nM (IC50) |
SMARCA4/BRG1/BAF190A 262.5 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| AN3-CA | GI50 |
0.021 μM
Compound: 17a
|
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
>5 μM
Compound: 17a
|
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
0.005 μM
Compound: 17a
|
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
0.183 μM
Compound: 17a
|
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
0.749 μM
Compound: 17a
|
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| BaF3 | GI50 |
1.677 μM
Compound: 17a
|
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| J82 | GI50 |
0.547 μM
Compound: 17a
|
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
| KMS-11 | GI50 |
0.034 μM
Compound: 17a
|
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
|
[PMID: 35436119] |
Chemical Information
-
CAS No. 2640217-64-5
-
Masse moléculaire 584.50
-
Formule C27H31Cl2N9O2
-
SMILES
CC(N1CCC(N2N=CC(NC3=NC(C4=CC=CN=C4NC5=C(Cl)C(OC)=CC(OC)=C5Cl)=NC=N3)=C2)CC1)C
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)