2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR Apoptosis
  4. 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.

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FGFR-IN-8 Chemical Structure

FGFR-IN-8 Chemical Structure

CAS No. : 2640217-64-5

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FGFR-IN-8 Related Antibodies

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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Description

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[1].

IC50 & Target

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)

V561M-FGFR1

262.5 nM (IC50)

Cellular Effect
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]
Molecular Weight

584.50

Formula

C27H31Cl2N9O2
CAS No.
SMILES

CC(N1CCC(N2N=CC(NC3=NC(C4=CC=CN=C4NC5=C(Cl)C(OC)=CC(OC)=C5Cl)=NC=N3)=C2)CC1)C
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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FGFR-IN-8 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:

FGFR-IN-82640217-64-5FGFRApoptosisFibroblast growth factor receptorBa/F3anticancerorally activeInhibitorinhibitorinhibit

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