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NVP-AEW541

NVP-AEW541

产品编号 T6080   CAS 475489-16-8
别名: AEW541

NVP-AEW541 (AEW541) 是一种IGF-1R 抑制剂,IC50为 0.15 μM。它也抑制InsR,IC50为 0.14 μM。

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NVP-AEW541 Chemical Structure
NVP-AEW541, CAS 475489-16-8
规格 价格/CNY 货期 数量
1 mg ¥ 495 现货
2 mg ¥ 727 现货
5 mg ¥ 1,230 现货
10 mg ¥ 1,980 现货
25 mg ¥ 3,420 现货
50 mg ¥ 4,870 现货
1 mL * 10 mM (in DMSO) ¥ 1,370 现货
其他形式的 NVP-AEW541:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: NVP-AEW541 (T6080)
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纯度: 99.55%
纯度: 98.7%
纯度: 96.03%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.
靶点活性 IGF-1R:0.15 μM, Insulin receptor:0.14 μM
体外活性 NVP-AEW541 also inhibits InsR, Tek, Flt1 and Flt3 with IC50 of 140 nM, 530 nM, 600 nM and 420 nM in purified kinases/recombinant kinase domains assay. NVP-AEW541 is more selective and shows 27-fold more potent than InsR at the cellular level. NVP-AEW541 suppresses the IGF-I-mediated survival, soft agar and proliferation of MCF-7 cells with IC50 of 0.162 μM, 0.105 μM and 1.64 μM, respectively. NVP-AEW541 also reduces the level of phospho-IGF-1R and phospho-PKB in NWT-21 cells. [1] NVP-AEW541 shows growth inhibitory effect on TC-71 musculoskeletal sarcoma cells in low-serum medium as well as in 10% FBS–containing medium. NVP-AEW541 inhibits cell cycle progression and induces specific G1 arrest in sarcoma cell lines (TC-71, SK-N-MC, SaoS-2, RD/18 and RH4). [2] NVP-AEW541 could inhibit the growth of human neuroblastoma cells with IC50 of 0.4-6.8 μM. An increase in the hypodiploid fraction and the depletion of the S and G2-M compartments could be detected in these cell lines. NVP-AEW541-driven inhibition of IGF-1R causes a reduction of phosphorylation of Akt, but not of Erk1 and Erk2 in neuroblastoma cells. [3] NVP-AEW541 inhibits glioma cell growth and disrupts the autocrine loop initiated by HIF1α stabilization. [4] A recent study shows that NVP-AEW541 suppresses the proliferation and viability of PC3, DU145, and 22Rv1 prostate cancer cells, without necessarity of associated cell death. NVP-AEW541 decreases phospho-Akt levels in 22Rv1 and DU415 cells but not PC3 cells, without affecting total Akt levels, which shows that PTEN status could determine the effectiveness of NVP-AEW541 with essential Akt. NVP-AEW541-induced radiosensization is dependent on Akt activation status. NVP-AEW541 could increase the H2AX phosphorylation (a measure of DSBs) in PC3, DU145, and 22Rv1 cells. [5]
体内活性 NVP-AEW541 (50 mg/kg, p.o.) results in abrogation of basal and IGF-I-induced receptor, and PKB and MAPK phosphorylation, with T/C value of 14% in the NWT-21 tumor xenograft. [1] NVP-AEW541 (50 mg/kg) causes tumor shrinkage in both HTLA-230 and SK-N-BE2c xenografts, without signs of systemic toxicity. NVP-AEW541 could inhibit tumor invasion both in Matrigel-coated chambers and in HTLA-230 xenografts. [3]
激酶实验 In vitro kinase assays: NVP-AEW541 is dissolved in DMSO (10 mM) and stored at -20 °C. Dilutions are freshly made in DMSO/water 1:1. The final concentration of DMSO in the enzyme assays is <0.5 %. The protein kinase assays are carried out in 96-well plates at RT and terminated by the addition of 20 μL of 125 mM EDTA. Subsequently, 30 μL (c-Abl, c-Src, IGF-1R) of the reaction mixture are transferred onto Immobilon-PVDF presoaked for 5 min with methanol, rinsed with water, then soaked for 5 min with 0.5 % H3PO4 and mounted on vacuum manifold. After spotting all samples, vacuum is connected and each well rinsed with 200 μL 0.5 % H3PO4. Membranes are removed and washed 4&times; on a shaker with 1.0 % H3PO4, once with ethanol. After drying, mounting in Packard TopCount 96-well frame, and adding of 10 μL/well of Microscint, membranes are counted. IC50 values are calculated by linear regression analysis of the percentage inhibition of NVP-AEW541 in duplicate, at four concentrations (usually 0.01, 0.1, 1, and 10 μM). One unit of protein kinase activity is defined as 1 nmol of 33P transferred from [γ33P]ATP to the substrate protein per minute per mg of protein at 37 °C.
细胞实验 Between 3 &times; 103 and 6 &times; 103 cells/well are seeded in 96-well plates with a total media volume of 100 μL/well. Increasing concentrations of NVP-AEW541 is added 24 hours thereafter in quadruplicate. 72 hours later, cells are fixed by addition of 25 μL/well Glutaraldehyde (20%) and incubation for 10 min at RT. Cells are then washed 2&times; with 200 μL/well Water and 100 μL Methylene Blue (0.05%) is added. After incubation for 10 min at RT, cells are washed 3&times; with 200 μL/well Water. 200 μL/well HCl (3%) is added, and following incubation for 30 min at RT on a plate shaker, absorbance is measured at 650 nm.(Only for Reference)
别名 AEW541
分子量 439.55
分子式 C27H29N5O
CAS No. 475489-16-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 51 mg/mL(116 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2751 mL 11.3753 mL 22.7505 mL 56.8764 mL
5 mM 0.455 mL 2.2751 mL 4.5501 mL 11.3753 mL
10 mM 0.2275 mL 1.1375 mL 2.2751 mL 5.6876 mL
20 mM 0.1138 mL 0.5688 mL 1.1375 mL 2.8438 mL
50 mM 0.0455 mL 0.2275 mL 0.455 mL 1.1375 mL
100 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL

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TargetMol Library Books参考文献

1. García-Echeverría C, et al. Cancer Cell. 2004, 5(3), 231-239. 2. Scotlandi K, et al. Cancer Res, 2005, 65(9), 3868-3876. 3. Tanno B, et al. Clin Cancer Res. 2006, 12(22), 6772-6780. 4. Gariboldi MB, et al. Biochem Pharmacol, 2010, 80(4), 455-462. 5. Isebaert SF, et al. Int J Radiat Oncol Biol Phys, 2011, 81(1), 239-247.

TargetMol Library Books文献引用

1. Lin W, Niu R, Park S M, et al.IGFBP5 is an ROR1 ligand promoting glioblastoma invasion via ROR1/HER2-CREB signaling axis.Nature Communications.2023, 14(1): 1578.
CHMFL-FLT3-122 Tandutinib Dovitinib Sorafenib 5'-Fluoroindirubinoxime Nintedanib PF 477736 A-443654

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 激酶抑制剂库 药物功能重定位化合物库 抗癌活性化合物库 抑制剂库 酪氨酸激酶分子库 抗癌临床化合物库 抗衰老化合物库 抗肺癌化合物库 已知活性化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

NVP-AEW541 475489-16-8 Angiogenesis Autophagy Tyrosine Kinase/Adaptors IGF-1R Tyrosine Kinases FLT AEW 541 Inhibitor Insulin Receptor AEW-541 NVPAEW541 inhibit NVP-AEW-541 NVP AEW541 AEW541 NVP-AEW 541 inhibitor

 

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