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

ISM7594 是一种具有口服活性的 FGFR2/3 抑制剂。ISM7594 在 FGFR2 或 FGFR3 改变的癌细胞系中显示出广谱抗增殖能力，包括 FGFR2/3 扩增、融合和突变 (BaF3-TEL-FGFR2-V564F (IC50 = 0.067 nM), BaF3-TEL-FGFR2-V564I (IC50 = 2 nM)) 类型。ISM7594 以剂量依赖性方式抑制肿瘤生长。ISM7594 可用于具有 FGFR2/3 异常的晚期实体瘤的研究。

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ISM7594

ISM7594 Chemical Structure

CAS No. : 3025799-76-9

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ISM7594 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

ISM7594 (0.01-1000 nM) 对 FGFR2 (IC50 = 1.7 nM) 和FGFR3 (IC50= 12.4 nM) 的抑制活性显著优于对照 RE1的活性[1]。
ISM7594 (0.01-1000 nM) 对多种 FGFR2 突变体显示出强大的抑制活性，包括V564I (IC50 = 4.4 nM) 和 V564F (IC50 = 0.22 nM)[1]。
ISM7594 在 Caco-2 试验中显示出较高的上皮渗透性和较低的外排比率[1]。
ISM7594 (0.152-1000 nM，2 h) 有效抑制胃腺癌 (SNU-16) 和膀胱癌 (RT4) 细胞中 FGFR 和 ERK 的磷酸化[1]。
ISM7594 (10 μM，72 h) 在 FGFR2/3 突变的 BaF3 细胞包括 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)；胃癌细胞包括 KATO-III (IC50 = 3.97 nM)、SNU-16 (IC50 = 1.6 nM)、SNU1 (IC50 = 3.69 nM)；乳腺癌细胞包括 SUM52PE (IC50 = 5.5 nM)、MCF-7 (IC50 = 8.77 μM)；子宫内膜癌细胞包括 AN3CA (IC50 = 7.18 nM)、MFE280 (IC50 = 73.7 nM)；膀胱癌细胞包括 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)；多发性骨髓瘤细胞包括 OPM-2 (IC50 = 81.6 nM)、U266 (IC50 = 5.28 μM)；肝癌细胞包括 Li-7 (IC50 = 2.34 μM) 中显示出抗增殖作用[1]。
ISM7594 (1000 nM) 对 FGFR1 表现出选择性抑制，抑制率为92.9%[1]。

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

ISM7594 相关抗体:

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.
体内研究
(In Vivo)

ISM7594 (3-30 mg/kg，灌胃，每日一次或两次，持续 21 天) 在 FGFR2 或 FGFR3 驱动的细胞衍生皮下移植瘤小鼠模型中以剂量依赖性方式抑制肿瘤生长[1]。

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.
分子量

540.52

Formula

C29H22F2N6O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ISM7594 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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