2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. SSR128129E free acid

SSR128129E free acid  (Synonyms: SSR free acid)

目录号: HY-15599A
产品使用指南

摩尔计算器

SSR128129E free acid 是口服可用的 FGFR 变构调节剂， 对FGFR1 的 IC50 值为1.9 μM。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 SSR128129E 通常具有更好的水溶性和稳定性。

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SSR128129E free acid Chemical Structure

SSR128129E free acid Chemical Structure

CAS No. : 848463-13-8

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SSR128129E free acid 的其他形式现货产品:

Other Forms of SSR128129E free acid:

SSR128129E free acid 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.

IC50 & Target[1]

FGFR1

1.9 μM (IC50)

FGFR2

 

FGFR3

 

FGFR4

 

体外研究
(In Vitro)

SSR128129E inhibits FGF2-induced EC proliferation with an IC50 of 31±1.6 nM, migration with an IC50 of 15.2±4.5 nM, and lamellipodia formation in a dose dependent manner. SSR128129E inhibits responses mediated by FGFR1-4. For instance, SSR128129E blocks EC migration in response to FGF1, a ligand of FGFR1 and FGFR4, and capillary tube formation in response to FGF19, a ligand of FGFR4. Proliferation and migration of the murine pancreatic Panc02 tumor cell line in response to FGF7 are also blocked by SSR128129E, showing that SSR128129E inhibits FGFR subtypes of other species as well. SSR128129E blocks different FGFR subtypes in various cell lines with nanomolar potency[1].

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

SSR128129E free acid 相关抗体:
体内研究
(In Vivo)

Oral delivery of SSR128129E (30 mg/kg/day, from day 3) inhibits growth of orthotopic Panc02 tumors by 44% and delays growth of Lewis lung carcinoma. oral SSR128129E (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E inhibits the growth of subcutaneous CT26 colon tumors by 34% and of the multidrug resistant MCF7/ADR breast cancer xenograft model by 40%. SSR128129E reduces tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes[1].

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

324.33

Formula

C18H16N2O4
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
Cell Assay
[1]

HUVECs, freshly isolated from different donors and used between passage two and five, are cultured in M199 medium supplemented with 20% fetal bovine serum (FBS), 2 mM L-glutamine, 30 mg/L endothelial cell growth factor supplements (EGCS), 10 units/mL heparin, and penicillin/streptomycin. For proliferation, ECs are starved overnight in growth factor-depleted M199 medium containing 2% FBS and stimulated for 24 hr with 10 ng/mL bFGF with SSR128129E or DMSO. Proliferation is assessed the last 2 hr by incubation with 1 μCi/mL [3H]thymidine[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice: Anesthetized BALB/c mice are inoculated with murine 4T1 mammary carcinoma cells. After randomization of tumor bearing mice for tumor size on day 5 after tumor cell inoculation, SSR128129E or vehicle (0.6 % methylcellulose) is administered daily via oral gavage at a dose of 30 mg/kg until the end of the experiment at day 21. Tumor volume is measured. At the end of the experiment, mice are sacrificed by pentobarbital injection, and lungs and tumors are dissected. Visible metastatic nodules on the lungs are counted by using a dissecting microscope[1].

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

SSR128129E free acid 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

SSR128129E848463-13-8SSRFGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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