SU 5402
(Synonyms: 2-[(1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-4-甲基-1H-吡咯-3-丙酸,SU-5402; SU5402) 目录号 : GC14660
SU 5402是一种多靶点受体酪氨酸激酶抑制剂，对血管内皮生长因子受体2（VEGF-R2）和成纤维细胞生长因子受体1（FGF-R1）酪氨酸激酶活性的IC50分别为20nM和30nM。
Cas No.:215543-92-3
Sample solution is provided at 25 µL, 10mM.
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SU 5402 is a multi-targeted receptor tyrosine kinase inhibitor that inhibit against vascular endothelial growth factor receptor 2 (VEGF-R2) and fibroblast growth factor receptor 1 (FGF-R1) tyrosine kinase activity with IC50 values of 20 and 30nM, respectively[1]. SU 5402 also acts as a FGF-2 inhibitor with an IC50 value of 9µM and produces concentration-dependent reductions in FGF-2 enhancement of granule neuron survival[2].
In vitro, SU 5402 (10μM) pretreated human breast cancer T47D cells for 20min before 10ng/mL bFGF stimulation effectively blocked the binding of bFGF to its receptor FGFR, thereby inhibiting the activation of downstream signaling pathways induced by bFGF. SU 5402 indirectly affects the activation of the PI3K/Akt and MAPK signaling pathways by selectively inhibiting FGFR, thereby effectively suppressing bFGF induced hypoxia-inducible factor (HIF-1α) expression[3]. SU 5402 (20μM) applied on thyroid cancer FTC133 cells for 4h inhibited the phosphorylation of LDHA and PKM2, which was elevated in all analysed cancer subtypes[4]. SU 5402 (10μM) treatment on murine mesenchymal stem cell line C3H10T1/2 cells cultured in osteoblast medium for 2 weeks with 2,000pg/mL fibroblast growth factor 23 (FGF23) diminished the bone-derived effects of FGF23[5].
In vivo, SU 5402 (3μg; 1μL) injected into the lateral ventricle of ICR mice 1h prior to daily oral gavage of paeoniflorin (40mg/kg) for 7 days prevented the antidepressant effects of paeoniflorin and blocked the neuroinflammatory and neurogenic regulatory effects of paeoniflorin[6]. SU 5402 (25mg/kg/day) administrated into monocrotaline-induced pulmonary hypertension (PH) rat model via daily s.c. injection from day 21 to day 42 reversed established monocrotaline-induced PH in rats, decreased the values of pulmonary artery pressure, right ventricular hypertrophy, and peripheral artery muscularization to the levels observed in vehicle-treated rats[7].
References:
[1] Sun L, Liang C X, Tang F, et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999 Dec 16;42(25):5120-30.
[2] Skaper S D, Kee W J, Facci L, et al. The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects. J Neurochem. 2000 Oct;75(4):1520-7.
[3] Zhang C C, Yu J X, Li S F, et al. Effect of basic fibroblast growth factor on hypoxia-inducible factor (HIF)-1α expression (Exp) and HIF-1 transcription in breast Cancer cell through PI-3 K Akt signaling. Cytokine. 2025 Mar:187:156859.
[4] Kachel P, Trojanowicz B, Sekulla C, et al. Phosphorylation of pyruvate kinase M2 and lactate dehydrogenase A by fibroblast growth factor receptor 1 in benign and malignant thyroid tissue. BMC Cancer. 2015 Mar 18;15:140.
[5] Li Y, He X, Olauson H, Larsson T E, Lindgren U. FGF23 affects the lineage fate determination of mesenchymal stem cells. Calcif Tissue Int. 2013 Dec;93(6):556-64.
[6] Cheng J, Chen M, Wan H Q, et al. Paeoniflorin exerts antidepressant-like effects through enhancing neuronal FGF-2 by microglial inactivation. J Ethnopharmacol. 2021 Jun 28:274:114046.
[7] Izikki M, Guignabert C, Fadel E, et al. Endothelial-derived FGF2 contributes to the progression of pulmonary hypertension in humans and rodents. J Clin Invest. 2009 Mar;119(3):512-23.
SU 5402是一种多靶点受体酪氨酸激酶抑制剂，对血管内皮生长因子受体2（VEGF-R2）和成纤维细胞生长因子受体1（FGF-R1）酪氨酸激酶活性的IC50分别为20nM和30nM[1]。SU 5402还可作为FGF-2抑制剂，IC50为9µM，并呈浓度依赖性降低FGF-2对小脑颗粒神经元的促存活作用[2]。
在体外模型中，SU 5402 (10μM) 预处理人乳腺癌T47D细胞20min后再以10ng/mL bFGF刺激，可有效阻断bFGF与其受体FGFR结合，从而抑制bFGF诱导的下游信号通路激活。 SU 5402通过选择性抑制FGFR间接影响PI3K/Akt和MAPK信号通路的激活，从而有效抑制bFGF诱导的缺氧诱导因子 (HIF-1α) 表达[3]。 SU 5402(20μM)处理甲状腺癌FTC133细胞4h，可抑制在所有癌症亚型中升高的LDHA和PKM2的磷酸化[4]。 SU 5402 (10μM) 处理在含有2000pg/mL成纤维细胞生长因子23 (FGF23)成骨培养基中的小鼠间充质干细胞系C3H10T1/2细胞并培养2周，可减弱FGF23的骨源性效应[5]。
SU 5402 (3μg; 1μL) 在每日口服芍药苷 (40mg/kg) 前1h经侧脑室注射入ICR小鼠，共持续7天，可阻止芍药苷的抗抑郁效应，并阻断其神经炎症和神经发生调节作用[6]。 SU 5402 (25mg/kg/day) 从第21天至第42天通过每日皮下注射给予野百合碱诱导的肺动脉高压 (PH) 大鼠模型，可逆转已建立的野百合碱诱导的PH，使肺动脉压、右心室肥厚和外周动脉肌化降至与对照组相当的水平[7]。
| Cell experiment [1]: | |
Cell lines | Human breast cancer T47D cells |
Preparation Method | After serum starvation for 24h, T47D cells were pretreated with SU 5402 (10μM) for 20min and 10ng/mL bFGF was applied for 18h for stimulation. |
Reaction Conditions | 10μM; 20min |
Applications | SU 5402 effectively blocked the binding of bFGF to its receptor FGFR, thereby inhibiting the activation of downstream signaling pathways induced by bFGF. SU 5402 indirectly affects the activation of the PI3K/Akt and MAPK signaling pathways by selectively inhibiting FGFR, thereby effectively suppressing bFGFinduced hypoxia-inducible factor (HIF-1α) expression. |
| Animal experiment [2]: | |
Animal models | Adult male Wistar rats |
Preparation Method | Adult male Wistar rats (200–250g) were given monocrotaline (60mg/kg; s.c.), left untreated for 21 days, then randomly divided into 2 groups, of which one was treated with SU 5402 (25mg/kg) and the other given the vehicle, from day 21 to day 42. All treatments were given once a day by s.c. injection. |
Dosage form | 25mg/kg; s.c.; daily from day 21 to day 42 |
Applications | SU 5402 reversed established monocrotaline-induced pulmonary hypertension in rats, decreasing the values of pulmonary artery pressure, right ventricular hypertrophy, and peripheral artery muscularization to the levels observed in vehicle-treated rats. |
References: | |
| Cas No. | 215543-92-3 | SDF | |
| 别名 | 2-[(1,2-二氢-2-氧代-3H-吲哚-3-亚基)甲基]-4-甲基-1H-吡咯-3-丙酸,SU-5402; SU5402 | ||
| 化学名 | 3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid | ||
| Canonical SMILES | CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O | ||
| 分子式 | C17H16N2O3 | 分子量 | 296.33 |
| 溶解度 | ≥ 14.8 mg/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 | 3.3746 mL | 16.8731 mL | 33.7462 mL |
| 5 mM | 0.6749 mL | 3.3746 mL | 6.7492 mL |
| 10 mM | 0.3375 mL | 1.6873 mL | 3.3746 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。
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Quality Control & SDS
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- Purity: >98.00%
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