SU1498 (AG 1498)
(Synonyms: AG 1498; Tyrphostin SU 1498) 目录号 : GC33840
SU1498 (AG 1498)是一种有效的血管内皮生长因子受体2（VEGFR-2）抑制剂，IC50值为0.7μM。
Cas No.:168835-82-3
Sample solution is provided at 25 µL, 10mM.
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SU1498 (AG 1498) is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 value of 0.7μM [1]. SU1498 can inhibit alveolar formation and regulate capillary number in neonatal mice by inhibiting vascular endothelial growth factor receptor[2]. SU1498 has been widely used to inhibit mitochondrial energy production to regulate cancer cell viability[3].
In vitro, SU1498 treatment for 48h inhibited the growth of DU145 cells with an IC50 value of 2.19 ± 0.14μM[4]. Treatment of MS-1 cells with 5μg/ml SU1498 for 24h blocked VEGFR-2 signaling, resulting in a decrease in Ets-1 levels[5]. Treatment of U87 cells with 10µM SU1498 for 72 hours inhibited cell proliferation, induced an increase in the number of apoptotic cells and altered cell morphology[6].
In vivo, SU1498 treatment (1μg/μl; 1μg in 1μl DMSO) via intravitreal injection for 7 days can inhibit laser-induced ocular angiogenesis in mice[7]. One month after subcutaneous injection of a single dose of SU1498 (30mg/kg) into the back of newborn mice, the development of renal tubules and glomerular was abnormal, accompanied by glomerular malformation, tubular dilation, and cell degeneration[8].
References:
[1] Boguslawski G, McGlynn P W, Harvey K A, et al. SU1498, an inhibitor of vascular endothelial growth factor receptor 2, causes accumulation of phosphorylated ERK kinases and inhibits their activity in vivo and in vitro[J]. Journal of Biological Chemistry, 2004, 279(7): 5716-5724.
[2] SJ C, CS G, JM S, et al. Su1498 Inhibits Alveolarization in Newborn Mice[J]. Pediatric Research, 2004, 56(4): 667-667.
[3] Kam Y, Winer L, Romero N. Screening of kinase inhibitors as bioenergetic metabolism modulator using the XF Real-Time ATP Rate Assay[J]. Cancer Research, 2023, 83(7_Supplement): 3969-3969.
[4] Kisielewska J, Ligeza J, Klein A. The effect of tyrosine kinase inhibitors, tyrphostins: AG1024 and SU1498, on autocrine growth of prostate cancer cells (DU145)[J]. Folia histochemica et cytobiologica, 2008, 46(2): 185-191.
[5] Arbiser J L, Larsson H, Claesson-Welsh L, et al. Overexpression of VEGF 121 in immortalized endothelial cells causes conversion to slowly growing angiosarcoma and high level expression of the VEGF receptors VEGFR-1 and VEGFR-2 in vivo[J]. The American journal of pathology, 2000, 156(4): 1469-1476.
[6] Mesti T, Savarin P, Triba M N, et al. Metabolic impact of anti-angiogenic agents on U87 glioma cells[J]. PloS one, 2014, 9(6): e99198.
[7] Shu-Ya T, Qiu-Yang Z, Jing-Jing L, et al. Suppression of pathological ocular neovascularization by a small molecule, SU1498[J]. Biomedicine & Pharmacotherapy, 2020, 128: 110248.
[8] Lee S J, Cho S J, Ju S Y, et al. Effect of retinoic acid on renal development in newborn mice treated with an angiogenesis inhibitor[J]. Pediatrics International, 2010, 52(3): 386-392.
SU1498 (AG 1498)是一种有效的血管内皮生长因子受体2（VEGFR-2）抑制剂，IC50值为0.7μM[1]。SU1498可通过抑制血管内皮生长因子受体，来抑制新生小鼠的肺泡形成并调节毛细血管数量[2]。SU1498已被广泛应用于通过抑制线粒体能量产生来调节癌细胞活力[3]。
在体外，使用SU1498处理DU145细胞48小时可抑制其生长，IC50值为2.19 ± 0.14μM[4]。用5μg/ml的SU1498处理MS-1细胞24小时，可阻断VEGFR-2信号传导，导致Ets-1水平降低[5]。用10µM的SU1498处理U87细胞72小时，能抑制细胞增殖、诱导凋亡细胞数量增加并改变细胞形态 [6]。
在体内，通过玻璃体内注射SU1498（1μg/μl；1μg溶于1μl DMSO）处理小鼠7天，可抑制激光诱导的眼部血管生成[7]。在新出生小鼠背部单次皮下注射SU1498（30mg/kg）一个月导致肾小管和肾小球的发育出现异常，并伴有肾小球畸形、肾小管扩张和细胞变性[8]。
| Cell experiment [1]: | |
Cell lines | DU145 cells |
Preparation Method | DU145 cells were seeded on 96-well plates at concentrations of 5×103cells/well in minimal essential medium (MEM) supplemented with 100IU/ml penicillin and 100mg/ml streptomycin in the presence of 10% FBS. Following 24h of incubation, the culture medium was replaced with serum-free DMEM/F12 (1:1) supplemented with transferrin (5mg/ml), sodium selenite (2ng/ml) and albumin (0.5mg/ml). After additional 24h of incubation (Day 0), the medium was replaced with serum-free DMEM/F12+ medium containing SU1498 (0.1, 1, 2, 4, 6, 8 and 10μM). The incubation was continued for the next 48h at 37°C in humidified atmosphere. Determine proliferation of DU145 cells. |
Reaction Conditions | 0.1, 1, 2, 4, 6, 8 and 10μM; 48h |
Applications | SU1498 treatment inhibited the cell viability of DU145 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male ddY mice |
Preparation Method | Male ddY mice (6 weeks of age) were fed and watered ad libitum and housed in a controlled environment (22±2°C, 50±5% humidity, 12-h light cycle starting at 07:00). The one vehicle group (n=5) received intraventricular injection of 5% dimethyl sulfoxide dissolved in 0.9% NaCl. In another vehicle-treated group, a single dose of SU1498 (25mM; 1ml) was intraventricular injected. Behavioral testing began 3 days after intraventricular injection. |
Dosage form | 25mM (1ml) for once; intraventricular injection |
Applications | SU1498 treatment impaired the memory of mice and caused recognition memory deficit. |
References: | |
| Cas No. | 168835-82-3 | SDF | |
| 别名 | AG 1498; Tyrphostin SU 1498 | ||
| Canonical SMILES | O=C(NCCCC1=CC=CC=C1)/C(C#N)=C/C2=CC(C(C)C)=C(O)C(C(C)C)=C2 | ||
| 分子式 | C25H30N2O2 | 分子量 | 390.52 |
| 溶解度 | DMSO：78 mg/mL (199.73 mM) ; Ethanol：78 mg/mL (199.73 mM) ; Water：Insoluble | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5607 mL | 12.8034 mL | 25.6069 mL |
| 5 mM | 512.1 μL | 2.5607 mL | 5.1214 mL |
| 10 mM | 256.1 μL | 1.2803 mL | 2.5607 mL |
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| 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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