WHI-P154
作者：齊岳
發(fā)布時間：2023-08-23
09:38:06
點擊數(shù)：
產品名稱：WHI-P154
產品描述：
| 產品描述 | WHI-P154 is a potent JAK3 inhibitor. |
| 靶點活性 | EGFR:4 nM, VEGFR:100 nM, JAK3:1.8 μM, Src:100 nM |
| 體外活性 | 體內使用EGF-P154導致嚴重聯(lián)合免疫缺陷小鼠成膠質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. |
| 體內活性 | WHI-P154的體外抗膠質母細胞瘤活性擴增> 200倍,并通過結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,并誘導人成膠質細胞瘤細胞系中的細胞凋亡。WHI-P154在ECM中抑制膠質母細胞瘤細胞粘附和遷移。 WHI-P154 對人惡性膠質瘤細胞系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。 |
| 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. |
| 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) |
| 別名 | Jak3 inhibitor ii |
| 分子量 | 376.21 |
| 分子式 | C16H14BrN3O3 |
| CAS No. | 211555-04-3 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 37.6 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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