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Enzastaurin (LY317615),Enzastaurin (LY317615)
  • Enzastaurin (LY317615),Enzastaurin (LY317615)

170364-57-5Enzastaurin (LY317615)

價格 詢價
包裝 1盒
最小起訂量 1盒
發(fā)貨地 上海
更新日期 2024-12-25
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產(chǎn)品詳情

中文名稱:Enzastaurin (LY317615)英文名稱:Enzastaurin (LY317615)
CAS:170364-57-5品牌: 一研
保存條件: Store at -20°C產(chǎn)品類別: 抑制劑
Cas : 170364-57-55
2024-12-25 Enzastaurin (LY317615) Enzastaurin (LY317615) 1盒/RMB 一研 Store at -20°C 抑制劑

產(chǎn)品屬性:

產(chǎn)品名稱

規(guī)格

CAS

型號

Enzastaurin (LY317615)

10mM (in 1mL DMSO) 5mg 25mg 100mg 500mg 1g

170364-57-5

EY-Y0165375

Cas No.170364-57-5

別名 N/A

化學(xué)名 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione

分子式 C32H29N5O2

Enzastaurin (LY317615).png

分子量 515.61

溶解度 8.6 mg/mL in DMSO

儲存條件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
Enzastaurin is an ATP-competitive, selective oral inhibitor of protein kinase Cβ with IC50 value of 6 nM [1].

Protein kinase C (PKC) is a family of serine-threonine protein kinases that have been proved to play critical roles in the formation and progression of tumor cells. The PKCβ is especially found to contribute to the growth and proliferation of tumors such as diffuse large B-cell lymphoma, multiple myeloma and chronic lymphoid leukemia. The selective PKCβ inhibitor enzastaurin was found to have antiangiogenic activity in tumor model as well as suppress tumor proliferation and induce apoptosis. Besides that, enzastaurin showed the inhibitory effects on phosphorylation of ribosomal protein S6, GSK3β and AKT which are in pathways influenced by PKC. Due to these, enzastaurin was developed as a therapy for cancer [1 and 2].

Enzastaurin at low concentration suppressed cell proliferation of various tumor cells including colon carcinoma (HCT-116), glioblastoma (U87MG), non–small cell lung cancer (A549), melanoma (M14), ovarian cancer (OVCAR-3), breast cancer (MCF-7), leukemia (K562), prostate cancer (PC-3), renal cancer (CAKI-1) and central nervous system cancer (U251). Enzastaurin induced apoptosis of tumor cells at low concentration in a range of 1 to 4 μM and the apoptosis was proved to be caspase-independent. In addition, enzastaurin suppressed the phosphorylation ofGSK3βSer9, ribosomal protein S6Ser240/244 and AKTThr308 time-dependently in tumor cells and affected these pathways [1 and 3].

In mice models, oral administration of enzastaurin at a dose of 75 mg/kg resulted in significant proliferation inhibition of U87MG glioblastoma or HCT116 coloncarcinoma xenografts. In mice bearing human walden strommacro globulinemia xenografts, administration of enzastaurin at dose of 80 mg/kg significantly reduced tumor growth of WM and increased survival [1 and 2].

Reference:

[1] Graff J R, McNulty A M, Hanna K R, et al.  The protein kinase Cβ–selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Research, 2005, 65(16): 7462-7469.

[2] Moreau A S, Jia X, Ngo H T, et al.  Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenstr mmacroglobulinemia. Blood, 2007, 109(11): 4964-4972.

[3] Rizvi M A, Ghias K, Davies K M, et al.  Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. Molecular cancer therapeutics, 2006, 5(7): 1783-1789.


關(guān)鍵字: 170364-57-5;C32H29N5O2;Enzastaurin (LY31761;

公司簡介

上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè),公司自成立以來,秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念,立足生物科技領(lǐng)域,運用生物技術(shù)和科研試劑,發(fā)展現(xiàn)代生物科技,為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品,服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。 公司具有對普通貨物、冷藏及冷凍倉庫的存儲、包裝及運輸能力。 公司將始終堅持信譽立業(yè)、以人為本、質(zhì)量保證、誠信服務(wù)的宗旨,不斷拼搏,開拓進取,與各界朋友攜手共創(chuàng)美好未來。
成立日期 2014-06-05 (11年) 注冊資本 100
員工人數(shù) 50-100人 年營業(yè)額 ¥ 100萬以內(nèi)
主營行業(yè) 生化試劑,抗體,細(xì)胞培養(yǎng),分子生物學(xué),免疫安全 經(jīng)營模式 工廠,試劑
  • 上海一研生物科技有限公司
VIP 3年
  • 公司成立:11年
  • 注冊資本:100
  • 企業(yè)類型:營業(yè)執(zhí)照
  • 主營產(chǎn)品:、ELISA試劑盒、PCR檢測試劑盒、生化檢測試劑盒、標(biāo)準(zhǔn)品、抗體、細(xì)胞等
  • 公司地址:上海市閔行區(qū)莘福路2號樓
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