store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NVP-HSP990 (HSP990) 是一种选择性的Hsp90抑制剂,对 Hsp90α、Hsp90β 和 Grp94 的IC50值分别为 0.6、0.8 和 8.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 622 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,490 | 现货 | ||
100 mg | ¥ 4,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 959 | 现货 |
产品描述 | NVP-HSP990 (HSP990) is an effective and specific HSP90α/β inhibitor (IC50: 0.6 /0.8 nM). |
靶点活性 | HSP90 β:0.8 nM, HSP90 α:0.6 nM |
体外活性 | NVP-HSP990 is based on a 2-amino-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one scaffold, which is structurally distinct from other known HSP90 inhibitors. NVP-HSP990 binds to the N-terminal ATP-binding domain of HSP90. NVP-HSP990 exhibits single digit nanomolar IC50 values on three of the HSP90 isoforms (HSP90α, HSP90β, and GRP94) and 320 nM IC50 value on the fourth (TRAP-1), with selectivity against unrelated enzymes, receptors, and kinases. NVP-HSP990 dissociates the HSP90-p23 complex, depleted client protein c-Met, and induced Hsp70 in c-Met amplified GTL-16 gastric tumor cells. NVP-HSP990 potently inhibites the growth of human cell lines and primary patient samples from a variety of tumor types. [1] NVP-HSP990 displays dose- and time-dependent effects on HSP90 client proteins. NVP-HSP990 inhibits Glioma tumor-initiating cells (GIC) proliferation in all GIC lines, with IC50 values ranging approximately between 10 and 500 nM. Olig2 is a functional marker associated with cell proliferation and response to NVP-HSP990, as NVP-HSP990 attenuated cell proliferation in Olig2-high GIC lines. In addition, NVP-HSP990 disrupted cell-cycle control mechanism by decreasing CDK2 and CDK4 and elevating apoptosis-related molecules. [2] |
体内活性 | NVP-HSP990 exhibits drug-like pharmaceutical and pharmacologic properties with high oral bioavailability. In the GTL-16 xenograft model, a single oral administration of 15 mg/kg of NVP-HSP990 induced sustained downregulation of c-Met and upregulation of Hsp70. In repeat dosing studies, NVP-HSP990 treatment resulted in tumor growth inhibition of GTL-16 and other human tumor xenograft models driven by well-defined oncogenic HSP90 client proteins. [1] |
激酶实验 | HSP90 binding, ATPase, and selectivity profiling assays: The potency of HSP90 inhibitors for HSP90α, HSP90β, and Grp94 is determined by AlphaScreen competition binding assays, and activity against TRAP-1 is assessed by an ATPase assay. |
细胞实验 | Dissociated GICs are plated at 10 cells/μL in 6-well plates and incubated with various concentrations of NVP-HSP990 for 7 days. Formed tumorspheres are dissociated into single cells and counted with hemocytometer using 0.2% Trypan blue exclusion. (Only for Reference) |
别名 | HSP990 |
分子量 | 379.39 |
分子式 | C20H18FN5O2 |
CAS No. | 934343-74-5 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 70 mg/mL (184.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6358 mL | 13.1791 mL | 26.3581 mL | 65.8953 mL |
5 mM | 0.5272 mL | 2.6358 mL | 5.2716 mL | 13.1791 mL | |
10 mM | 0.2636 mL | 1.3179 mL | 2.6358 mL | 6.5895 mL | |
20 mM | 0.1318 mL | 0.659 mL | 1.3179 mL | 3.2948 mL | |
50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3179 mL | |
100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.659 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
NVP-HSP990 934343-74-5 Apoptosis Cytoskeletal Signaling Metabolism HSP Heat shock proteins NVP HSP990 NVP-HSP 990 Inhibitor HSP 990 HSP-990 inhibit NVPHSP990 HSP990 NVP-HSP-990 inhibitor