| 名稱 | WHI-P154 |
| 描述 | WHI-P154 (Jak3 inhibitor ii) is a potent JAK3 inhibitor. |
| 細胞實驗 | Cells are seeded into a 96-well plate at a density of 2.5×104 cells/well and incubated for 36 h at 37 ℃ before drug exposure. On the day of treatment, culture medium is carefully aspirated from the wells and replaced with fresh medium containing the quinazoline compounds WHI-P154 at concentrations ranging from 0.1 μM to 250 μM. Triplicate wells are used for each treatment. The cells are incubated with the compound for 24hours to 36hours at 37 ℃ in a humidified 5% CO2 atmosphere. To each well, 10 μL of MTT (final concentration, 0.5 mg/mL) is added, and the plate are incubated at 37 ℃ for 4 h. Than solubilized overnight at 37 ℃ in a solution containing 10% SDS in 0.01 M HCL. The absorbance of each well is measured in a microplate reader at 570 nm.(Only for Reference) |
| 激酶實驗 | Kinase assays: WHI-P154 is tested in kinase assays. The panel of kinases is selected to broadly cover the kinome, providing a good approximation of specificity. For all kinases, recombinant rat (IKKβ) or human (all others), full-length or GST-kinase domain fusion proteins, are used. WHI-P154 is inactive (concentration that inhibits response by 50% [IC50] > 30 μM) for the following kinases: AKT, AuroraA, cdk2, cdk6, CHK1, FGFR1, GSK3b, IKKb, IKKi, INSR, MAPK1, MAPKAP-K2, MASK, MET, PAK4, PDK1, PKCb, ROCK1, TaoK3, TrkA. |
| 體外活性 | 體內(nèi)使用EGF-P154導致嚴重聯(lián)合免疫缺陷小鼠成膠質(zhì)細胞瘤異種移植模型中的腫瘤生長延遲并且改善無瘤存活.然而無瘤小鼠生存期都沒有超過33天 (無瘤生存期中值為19天),并且所有對照小鼠的腫瘤在58天內(nèi)迅速達到平均尺寸> 500 mM3,用1 mg/kg/天 EGF-P154連續(xù)治療10天的小鼠中有40%活下來并且58天以上沒有檢測到腫瘤,無瘤生存期中值為40天.剩下的60%小鼠中腫瘤體積從未超過50 mm3. |
| 體內(nèi)活性 | WHI-P154的體外抗膠質(zhì)母細胞瘤活性擴增> 200倍,并通過結(jié)合重組人源表皮生長因子而具有選擇性。WHI-P154在體外抑制巨噬細胞中STAT1激活,iNOS表達和NO產(chǎn)生。研究證明,WHI-P154還可以抑制其它常見激酶,包括EGFR,Src,Abl,VEGFR,MAPK和PI3-K,并誘導人成膠質(zhì)細胞瘤細胞系中的細胞凋亡。WHI-P154在ECM中抑制膠質(zhì)母細胞瘤細胞粘附和遷移。 WHI-P154 對人惡性膠質(zhì)瘤細胞系U373和U87具有明顯的細胞毒性,在微摩爾濃度下引起凋亡性細胞死亡。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (132.91 mM), Sonication is recommended.
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| 關(guān)鍵字 | Janus kinase | WHI-P-154 | WHI-P 154 | ErbB-1 | Apoptosis | inhibit | JAK | WHI-P154 | Epidermal growth factor receptor | HER1 | WHIP154 | Inhibitor | WHI P154 | EGFR |
| 相關(guān)產(chǎn)品 | L-Glutamic acid | Gefitinib | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
| 相關(guān)庫 | 抑制劑庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 抗前列腺癌化合物庫 |