| 名称 | SHP099 hydrochloride |
| 描述 | SHP099 hydrochloride is a potent, selective, orally bioavailable SHP2 inhibitor with IC50 of 70 nM, which inhibits ERK1/2 activation in cancer cells. [2] |
| 细胞实验 | Cells are plated onto 96-well plates in 100 μL medium. SHP099 with various concentrations (1.25, 2.5, 5, 10, 20 μM) are added 24 h after cell plating. At day 5, 50 μL Celltiter-Glo reagent is added, and the luminescent signal is determined[1]. |
| 激酶实验 | The inhibition of SHP2 from the tested compounds (SHP099) concentrations varying from 0.003-100 μM is monitored using an assay in which 0.5 nM of SHP2 is incubated with of 0.5 μM of peptide IRS1_pY1172(dPEG8)pY1222. After 30-60 minutes incubation at the surrogate substrate, DiFMUP is added to the reaction and incubated at 25 °C for 30 minutes. The reaction is then quenched by the addition of 5 μL of a 160 μM solution of bpV(Phen). The fluorescence signal is monitored using a microplate reader using excitation and emission wavelengths of 340 nm and 450 nm, respectively[1]. |
| 体外活性 | 方法：不同浓度的SHP099（5,10,15,20,25,30,40,50μM）处理1周后，观察SMSCs的细胞活力。
结果：SHP099在浓度大于25μM的时候抑制SMSCs的细胞活力。[2] |
| 体内活性 | 方法：用SHP0999(1,3,10mg/kg)处理了咪喹莫特 （IMQ）诱导的小鼠银屑病模型,观察SHP099对IMQ诱导的小鼠模型中的银屑病样表型的影响。
结果：SHP099显著抑制IMQ诱导的肿胀、表皮棘皮棘皮、角质形成细胞增殖和真皮炎症细胞浸润，不影响正常小鼠的皮肤状况；SHP099 也显著降低了小鼠模型中血清 IL-23 和 IL-17A 水平。[1]
方法：评估了 SHP099 在 400 μL 体积中以 100 mg/kg 口服单剂量 SHP099 后在 C57BL/6J 小鼠中穿过 BBB 的能力。
结果：口服强饲后早期血浆和脑组织中SHP099浓度较高，在口服强饲后24 h，脑组织中SHP099的水平保持在可观的水平。[2]
方法：CT-26 和 MC-38 细胞皮下接种到 BALB/c 小鼠中建立小鼠肿瘤模型，小鼠肿瘤模型使用SHP099盐酸盐（5mg/kg/kg/d，腹腔注射），观察SHP099盐酸盐第肿瘤的影响。
结果：SHP099治疗的肿瘤体积和重量均显著降低。[3] |
| 存储条件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2.5 mg/mL (6.43 mM), Sonication is recommeded.
Methanol : 15 mg/mL (38.59 mM), Sonication is recommended.
DMSO : 32 mg/mL (82.32 mM), Sonication and heating are recommended.
H2O : 10 mg/mL (25.73 mM), Sonication is recommended.
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| 关键字 | SHP-2 | SHP-099 Hydrochloride | SHP-099 hydrochloride | SHP099 Hydrochloride | SHP099 hydrochloride | SHP-099 | SHP099 | SHP 099 Hydrochloride | SHP 099 | Phosphatase | Inhibitor | inhibit |
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