2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. ISM7594

ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations.

For research use only. We do not sell to patients.

ISM7594 Chemical Structure

ISM7594 Chemical Structure

CAS No. : 3025799-76-9

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ISM7594 Related Antibodies

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Description

ISM7594 is an orally active FGFR2/3 inhibitor. ISM7594 shows broad-spectrum antiproliferative potency in FGFR2- or FGFR3-altered cancer cell panels, including FGFR2/3 amplification, fusion, and mutation (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) types. ISM7594 inhibits tumor growth in a dose-dependent manner. ISM7594 can be used for the study of advanced solid tumors with FGFR2/3 aberrations[1].

IC50 & Target

FGFR1

118.4 nM (IC50)

FGFR2

1.7 nM (IC50)

FGFR3

12.4 nM (IC50)

FGFR4

3066 nM (IC50)

In Vitro

ISM7594 (0.01-1000 nM) exhibits markedly superior inhibitory activities against FGFR2 (IC50 = 1.7 nM) and FGFR3 (IC50 = 12.4 nM) compared to the benchmark RE1[1].
ISM7594 (0.01-1000 nM) shows strong inhibitory activity against multiple FGFR2 mutants (V564I (IC50 = 4.4 nM), V564F (IC50 = 0.22 nM))[1]. ISM7594 demonstrates a higher epithelial permeability and a lower efflux ratio in the Caco-2 assay[1].
ISM7594 (0.152-1000 nM, 2 h) effectively suppresses the phosphorylation of FGFR and ERK in gastric adenocarcinoma (SNU-16) and bladder carcinoma (RT4) cells[1].
ISM7594 (10 μM, 72 h) demonstrates potent antiproliferative activity against in the gatekeeper mutant FGFR2/3 in BaF3 cells (BaF3-TEL-FGFR2 (IC50 = 0.17 nM), BaF3-TEL-FGFR3 (IC50 = 14 nM), BaF3-FGFR3-TACC (IC50 = 81 nM), BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM), BaF3-FGFR3-TACC3-G370C-K650E (IC50 = 34.7 nM)), gastric cancer cells (KATO-III (IC50 = 3.97 nM), SNU-16 (IC50 = 1.6 nM), SNU1 (IC50 = 3.69 nM)), breast cancer cells (SUM52PE (IC50 = 5.5 nM), MCF-7 (IC50 = 8.77 μM)), endometrial cancer cells (AN3CA (IC50 = 7.18 nM), MFE280 (IC50 = 73.7 nM)), bladder cancer cells (RT112-84 (IC50 = 19.8 nM), RT4 (IC50 = 13.9 nM), UM-UC-14 (IC50 = 71 nM), T24 (IC50 = 5.86 μM), UM-UC-3 (IC50 = 8.21 μM)), multiple myeloma (OPM-2 (IC50 = 81.6 nM), U266 (IC50 = 5.28 μM)) and liver cancer (Li-7 (IC50 = 2.34 μM))[1].
ISM7594 (1000 nM) selectively inhibits FGFR1, achieving a 92.9% inhibition rate[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ISM7594 Related Antibodies

Western Blot Analysis[1]

Cell Line: SNU-16 and RT4 cells
Concentration: 0, 0.152, 0.457, 1.372, 4.115, 12.34, 37.0, 111, 333, 1000 nM
Incubation Time: 2 h
Result: Suppressed the phosphorylation of FGFR (IC50 = 1.5 nM) and the phosphorylation of ERK (IC50 = 2.1 nM) in SNU-16 cells.
Suppressed the phosphorylation of ERK (IC50 = 22 nM) in RT4 cells.
In Vivo

ISM7594 (3-30 mg/kg, i.g., once or twice daily, 21 days ) inhibits tumor growth in a dose-dependent manner in FGFR2- or FGFR3-driven cell-derived subcutaneous xenograft mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SNU-16 cells (10 million)-derived subcutaneous xenograft female Balb/c nude mice [1]
Dosage: 3, 10, 30 mg/kg
Administration: i.g. once or twice daily for 21 days
Result: Inhibited tumor growth in a dose-dependent manner without body weight loss or signs of toxicity.
Demonstrated significant p-FGFR2 suppression and moderate p-AKT suppression.
Animal Model: RT4 cells (10 million)-derived subcutaneous xenograft female Balb/c nude mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: i.g. once or twice daily for 21 days
Result: Inhibited tumor growth in a dose-dependent manner without body weight loss or signs of toxicity.
Molecular Weight

540.52

Formula

C29H22F2N6O3
CAS No.
SMILES

C=C(C(NC1=CC=C(C=C1)C2=C(C3=CC=C(C(F)=C3)OC4=NC=CC(C)=N4)C(C(N)=O)=C5C=C(C=NN52)C)=O)F
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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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ISM7594 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:

ISM75943025799-76-9ISM 7594ISM-7594FGFRFibroblast growth factor receptorFGFR2/3cancerSNU-16 cellsRT4 cellsInhibitorinhibitorinhibit

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