SSR128129E
(Synonyms: SSR) 目录号 : GC10491
An FGFR inhibitor
Cas No.:848318-25-2
Sample solution is provided at 25 µL, 10mM.
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SSR128129E is an allosteric inhibitor of FGFR1 with IC50 value of 1.9 μM [1].
The fibroblast growth factor receptors (FGFRs) are receptor tyrosine kinases for fibroblast growth factors (FGFs) and play an important role in cancer and inflammation. FGF2 plays an important role in angiogenesis [1] [2].
SSR128129E is an orally-active and allosteric FGFR1 inhibitor. In human umbilical venous endothelial cells (HUVECs), SSR128129E inhibited FGF2-induced endothelial cells (ECs) proliferation and migration with IC50 values of 31 and 15.2 nM respectively and also inhibited lamellipodia formation. SSR128129E inhibited responses mediated by FGFR1-4. In FGFR2-expressing HEK293 cells, SSR128129E inhibited phosphorylation of FRS2 and ERK1/2 induced by FGF2 [1].
In arthritis mice, SSR128129E inhibited bone and joint damage and reduced angiogenesis in the inflamed joints. In orthotopic Panc02 tumor model, SSR128129E (30 mg/kg) inhibited tumor growth by 44%. In murine 4T1 breast tumors, SSR128129E (30 mg/kg) reduced tumor weight and size by 40% and 53%, respectively [1]. In atherosclerosis-prone apolipoprotein E (apoE)-deficient mice, SSR128129E (50 mg/kg) reduced neointimal proliferation and reduced FGFR2 mRNA levels and lesion size in the aortic sinus [2].
References:
[1]. Bono F, De Smet F, Herbert C, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell, 2013, 23(4): 477-488.
[2]. Dol-Gleizes F, Delesque-Touchard N, Marès AM, et al. A new synthetic FGF receptor antagonist inhibits arteriosclerosis in a mouse vein graft model and atherosclerosis in apolipoprotein E-deficient mice. PLoS One, 2013, 8(11): e80027.
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Bono F, et al. Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties. Cancer Cell. 2013 Apr 15;23(4):477-88. | |
| Cas No. | 848318-25-2 | SDF | |
| 别名 | SSR | ||
| 化学名 | sodium;2-amino-5-(1-methoxy-2-methylindolizine-3-carbonyl)benzoate | ||
| Canonical SMILES | CC1=C(N2C=CC=CC2=C1OC)C(=O)C3=CC(=C(C=C3)N)C(=O)[O-].[Na+] | ||
| 分子式 | C18H15N2O4.Na | 分子量 | 346.31 |
| 溶解度 | ≥ 17.3mg/mL in DMSO | 储存条件 | Store at -20° C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8876 mL | 14.4379 mL | 28.8759 mL |
| 5 mM | 0.5775 mL | 2.8876 mL | 5.7752 mL |
| 10 mM | 0.2888 mL | 1.4438 mL | 2.8876 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet