WHI-P154
作者：齊岳
發(fā)布時(shí)間：2023-08-23
09:38:06
點(diǎn)擊數(shù)：
產(chǎn)品名稱：WHI-P154
產(chǎn)品描述：
| 產(chǎn)品描述 | WHI-P154 is a potent JAK3 inhibitor. |
| 靶點(diǎn)活性 | EGFR:4 nM, VEGFR:100 nM, JAK3:1.8 μM, Src:100 nM |
| 體外活性 | 體內(nèi)使用EGF-P154導(dǎo)致嚴(yán)重聯(lián)合免疫缺陷小鼠成膠質(zhì)細(xì)胞瘤異種移植模型中的腫瘤生長(zhǎng)延遲并且改善無(wú)瘤存活.然而無(wú)瘤小鼠生存期都沒(méi)有超過(guò)33天 (無(wú)瘤生存期中值為19天),并且所有對(duì)照小鼠的腫瘤在58天內(nèi)迅速達(dá)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(lái)并且58天以上沒(méi)有檢測(cè)到腫瘤,無(wú)瘤生存期中值為40天.剩下的60%小鼠中腫瘤體積從未超過(guò)50 mm3. |
| 體內(nèi)活性 | WHI-P154的體外抗膠質(zhì)母細(xì)胞瘤活性擴(kuò)增> 200倍,并通過(guò)結(jié)合重組人源表皮生長(zhǎng)因子而具有選擇性。WHI-P154在體外抑制巨噬細(xì)胞中STAT1激活,iNOS表達(dá)和NO產(chǎn)生。研究證明,WHI-P154還可以抑制其它常見(jiàn)激酶,包括EGFR,Src,Abl,VEGFR,MAPK和PI3-K,并誘導(dǎo)人成膠質(zhì)細(xì)胞瘤細(xì)胞系中的細(xì)胞凋亡。WHI-P154在ECM中抑制膠質(zhì)母細(xì)胞瘤細(xì)胞粘附和遷移。 WHI-P154 對(duì)人惡性膠質(zhì)瘤細(xì)胞系U373和U87具有明顯的細(xì)胞毒性,在微摩爾濃度下引起凋亡性細(xì)胞死亡。 |
| 激酶實(shí)驗(yàn) | 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(xì)胞實(shí)驗(yàn) | 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(chǔ)
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 )
聯(lián)系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷(xiāo)售等。涉及產(chǎn)品為通用試劑的分銷(xiāo)、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
主營(yíng)產(chǎn)品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉(zhuǎn)換、石墨烯、光電材料、點(diǎn)擊化學(xué)、凝集素、載玻片、蛋白質(zhì)交聯(lián)劑、脂質(zhì)體、蛋白、多肽、氨基酸、糖化學(xué)等。
