FGFR1-IN-19
FGFR1-IN-19 is a selective, orally active, irreversible, covalent FGFR1 inhibitor with an IC50 of 7.6 nM. FGFR1-IN-19 reduces the phosphorylation levels of PLCγ, AKT, and ERK. FGFR1-IN-19 induces G0/G1 phase arrest and Caspase-dependent Apoptosis. FGFR1-IN-19 can be used for research on FGFR1-amplified lung cancer.
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- CAS No.: 2991245-67-9
- Formule: C31H34N6O3
- Masse moléculaire:538.64
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Activité biologique
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Activité biologique
Description
FGFR1-IN-19 is a selective, orally active, irreversible, covalent FGFR1 inhibitor with an IC50 of 7.6 nM. FGFR1-IN-19 reduces the phosphorylation levels of PLCγ, AKT, and ERK. FGFR1-IN-19 induces G0/G1 phase arrest and Caspase-dependent Apoptosis. FGFR1-IN-19 can be used for research on FGFR1-amplified lung cancer[1].
IC50 & Target
[1]|
FGFR1 7.6 nM (IC50) |
FGFR2 300.1 nM (IC50) |
FGFR3 862.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DMS-53 | IC50 |
0.087 μM
|
Antiproliferative activity against human DMS53 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human DMS53 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| DMS-114 | IC50 |
0.021 μM
|
Antiproliferative activity against human DMS114 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human DMS114 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| NCI-H1581 | IC50 |
0.024 μM
|
Antiproliferative activity against human NCI-H1581 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human NCI-H1581 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| NCI-H520 | IC50 |
0.084 μM
|
Antiproliferative activity against human NCI-H520 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human NCI-H520 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| KATO III stomach cancer cell line | IC50 |
2.311 μM
|
Antiproliferative activity against human KATOIII cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human KATOIII cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| SNU-16 | IC50 |
1.074 μM
|
Antiproliferative activity against human SNU-16 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human SNU-16 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
|
Rational-Design-of-Potent-and-Highly-Selective |
| RT-4 | IC50 |
1.893 μM
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Antiproliferative activity against human RT4 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human RT4 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| NCI-H146 | IC50 |
20 μM
|
Antiproliferative activity against human NCI-H146 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
Antiproliferative activity against human NCI-H146 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
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Rational-Design-of-Potent-and-Highly-Selective |
| NCI-H446 | IC50 |
2.316 μM
|
Antiproliferative activity against human NCI-H446 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human NCI-H446 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| NCI-H69 | IC50 |
1.075 μM
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Antiproliferative activity against human NCI-H69 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human NCI-H69 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| A549 | IC50 |
20 μM
|
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
Antiproliferative activity against human A549 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
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Rational-Design-of-Potent-and-Highly-Selective |
| DU-145 | IC50 |
4.334 μM
|
Antiproliferative activity against human DU145 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human DU145 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| PC-3 | IC50 |
6.651 μM
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Antiproliferative activity against human PC-3 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human PC-3 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| PANC-1 | IC50 |
3.572 μM
|
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human PANC-1 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| A-375 | IC50 |
20 μM
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Antiproliferative activity against human A-375 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
Antiproliferative activity against human A-375 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
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Rational-Design-of-Potent-and-Highly-Selective |
| HCT-116 | IC50 |
6.751 μM
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Antiproliferative activity against human HCT116 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human HCT116 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| MDA-MB-231 | IC50 |
9.835 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| MV4-11 | IC50 |
5.471 μM
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Antiproliferative activity against human MV-4-11 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against human MV-4-11 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
| MKN-45 | IC50 |
20 μM
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Antiproliferative activity against human MKN-45 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
Antiproliferative activity against human MKN-45 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
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Rational-Design-of-Potent-and-Highly-Selective |
| VCaP | IC50 |
20 μM
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Antiproliferative activity against human VCaP cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
Antiproliferative activity against human VCaP cells assessed as viability reduction incubated 72 hrs by CCK-8 assay; IC50 greater than 20 μM.
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Rational-Design-of-Potent-and-Highly-Selective |
| Panc02 | IC50 |
4.274 μM
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Antiproliferative activity against mouse Pan02 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
Antiproliferative activity against mouse Pan02 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.
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Rational-Design-of-Potent-and-Highly-Selective |
In Vitro
Anti-cancerApoptosisCell Cycle RegulationOthers
Anti-cancer
FGFR1-IN-19 (Different concentrations; 72 h) is most potent in FGFR1-amplified lung cancer lines DMS114 (IC50 0.021 μM) and NCI-H1581 (0.024 μM), with weaker activity in FGFR2/3-amplified and FGFR-WT lines[1].
FGFR1-IN-19 (10-20 nM) decreases colony formation in FGFR1-amplified lung cancer cells[1].
FGFR1-IN-19 (10-20 nM) decreases colony formation in FGFR1-amplified lung cancer cells[1].
Cell Cycle Regulation
FGFR1-IN-19 (10-20 nM; 24 h) causes G0/G1 arrest in NCI-H1581 and DMS114 cells[1].
Others
FGFR1-IN-19 (Compound 24) is a potent FGFR1 inhibitor with IC50 7.6 nM and substantially weaker activity against FGFR2, FGFR3, and the L494M/C488S FGFR1 mutants[1].
FGFR1-IN-19 (0-60 min) covalently modifies FGFR1 at Cys488, with FGFR1-24 adduct formation increasing from 47.6% at 15 min to 91.1% at 60 min[1].
FGFR1-IN-19 most strongly inhibited FGFR1 in the 207-kinase panel, with lower inhibition of FGFR2, FGFR3, and FGFR4[1].
FGFR1-IN-19 has weak hERG inhibitory activity with an IC50 of 31668 nM[1].
FGFR1-IN-19 (0-100 nM; 12 h and 0-24 h) blocks FGFR1 signaling in NCI-H1581 and DMS114 cells by reducing p-FGFR1, p-PLCγ, p-AKT, and p-ERK[1].
FGFR1-IN-19 (10-20 nM; 48 h) reduces migration and invasion of NCI-H1581 and DMS114 cells[1].
FGFR1-IN-19 (0-60 min) covalently modifies FGFR1 at Cys488, with FGFR1-24 adduct formation increasing from 47.6% at 15 min to 91.1% at 60 min[1].
FGFR1-IN-19 most strongly inhibited FGFR1 in the 207-kinase panel, with lower inhibition of FGFR2, FGFR3, and FGFR4[1].
FGFR1-IN-19 has weak hERG inhibitory activity with an IC50 of 31668 nM[1].
FGFR1-IN-19 (0-100 nM; 12 h and 0-24 h) blocks FGFR1 signaling in NCI-H1581 and DMS114 cells by reducing p-FGFR1, p-PLCγ, p-AKT, and p-ERK[1].
FGFR1-IN-19 (10-20 nM; 48 h) reduces migration and invasion of NCI-H1581 and DMS114 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
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Cell Line:22 cell lines
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Concentration:Different concentrations
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Incubation Time:72 h (compound incubation); 3-4 h (CCK-8 incubation)
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Result:IC50 values were DMS53 0.087 μM; DMS114 0.021 μM; NCI-H1581 0.024 μM; NCI-H520 0.084 μM; KATOIII 2.311 μM; SNU-16 1.074 μM; RT4 1.893 μM; NCI-H146 >20 μM; NCI-H446 2.316 μM; NCI-H69 1.075 μM; A549 >20 μM; DU145 4.334 μM; PC-3 6.651 μM; 22RV1 5.196 μM; PANC-1 3.572 μM; A-375 >20 μM; HCT116 6.751 μM; MDA-MB-231 9.835 μM; MV-4-11 5.471 μM; MKN-45 >20 μM; VCaP >20 μM; Pan02 4.274 μM.
Western Blot Analysis[1]
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Cell Line:NCI-H1581 and DMS114 cells
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Concentration:0, 3, 10, 30, and 100 nM
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Incubation Time:12 h (concentration response); 0, 3, 6, 9, 12, and 24 h (time course)
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Result:Reduced phosphorylation of FGFR1 and downstream effectors PLCγ, AKT, and ERK in a dose- and time-dependent manner in NCI-H1581 and DMS114 cells.
Cell Cycle Analysis[1]
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Cell Line:NCI-H1581 and DMS114 cells
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Concentration:10 and 20 nM
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Incubation Time:24 h
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Result:Induced G0/G1 cell-cycle arrest and decreased the proportion of cells in S and G2/M phases.
Apoptosis Analysis[1]
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Cell Line:NCI-H1581 and DMS114 cells
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Concentration:50 and 100 nM
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Incubation Time:72 h
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Result:Triggered apoptosis in a concentration-dependent manner in NCI-H1581 and DMS114 cells.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H1581 xenografts[1]
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Dosage:12.5 mg/kg
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Administration:p.o.; single dose
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Result:Intratumoral p-FGFR1 was downregulated at 2 h, and inhibition persisted to 12 h after the single 12.5 mg/kg oral dose.
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Animal Model:Balb/c NuNu (female, 6-8 weeks)[1]
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Dosage:12.5 mg/kg and 25 mg/kg
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Administration:daily; 16 consecutive days
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Result:At 25 mg/kg and 12.5 mg/kg, tumor growth was suppressed.
Western blot and immunohistochemistry showed reduced p-FGFR1 and Ki-67 in tumor tissues.
Related Protocols :
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
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CAS No. 2991245-67-9
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Masse moléculaire 538.64
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Formule C31H34N6O3
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SMILES
C=CC(N1CC(CN(CC2=CC=C(N3C=C(C4=CC(OC)=CC(OC)=C4)C5=CN=C(NC)N=C53)C=C2)C6)C6C1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Select Batch:
Pureté:
99.98%
Assay:
99.98%
ee.:
99.98%
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FGFR1-IN-19 Related Classifications
HY-191441 Related Classifications
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