產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
ENMD-2076 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg | 934353-76-1 | EY-Y0165366 |
Cas No.934353-76-1
別名
化學名 6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine
分子式 C21H25N7
分子量 375.47
溶解度 ≥ 18.75 mg/mL in DMSO, ≥ 2.55 mg/mL in EtOH with ultrasonic
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：
ENMD-2076 is a selective inhibitor of Aurora A and Flt3 with IC50 value of 14 and 1.86 nM[1].
Aurora kinases contains aurora A, aurora B and aurora C. They are serine/threonine kinases witch play an important role in cell proliferation. Aurora kinases are essential for cellular division by controlling segregation of chromatid. Aurora A is required for correct function of the centrosomes during the prophase of mitosis [1]. VEGFR (VEGF receptors) are receptors for VEGF (vascular endothelial growth factor). There are VEGFR 1, 2 and 3 which three main subtypes of VEGFR. The VEGFRs are tyrosine kinase receptors which are activited by binding to VEGFs then mediate the cellular responses to VEGF including the formation of the circulatory system (vasculogenesis) and the growth of blood vessels(angiogenesis) [1].
ENMD-2076 indicates activities of RET, FLT3, FLT4/VEGFR3, SRC, CSF1R/FMS, NTRK1, FGFR1/2, VEGFR2/KDR, LCK, and PDGFRα which all are kinases involved in angiogenes with IC50 from 1.86-120 nM. ENMD-2076 can inhibit the growth of hematopoietic cancer cell lines and lots of solid tumor with IC50 values from 25 to 700 nM in vitro[1]. ENMD-2076 significantly caused cytotoxicity in multiple myeloma (MM) cell lines and primary cells. ENMD-2076 also inhibited the phosphoinositide 3-kinase (PI3K)/AKT pathway. ENMD-2076 also induced cell cycle arrest in G2/M phase by inhibiting the activities of aurora kinases containing A and B class.[2]
ENMD-2076 regresses formed vessels and prevents new blood vessels formation in tumorxenograft models. [1] ENMD-2076 resulted in inhibition of tumour growth with oral treatment a dose-dependent manner with 50, 100, 200 mg/kg per day with human plasmacytoma xenografts[2].
References:
[1]. Fletcher GC, Brokx RD, Denny TA, Hembrough TA, Plum SM, Fogler WE, Sidor CF, Bray MR: ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther 2011, 10(1):126-137.
[2]. Wang X, Sinn AL, Pollok K, Sandusky G, Zhang S, Chen L, Liang J, Crean CD, Suvannasankha A, Abonour R et al: Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol 2010, 150(3):313-325.
關鍵字： 934353-76-1;C21H25N7;ENMD-2076;
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、分子生物學和常規(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""全心全意服務于科研工作者""的企業(yè)理念，立足生物科技領域，運用生物技術和科研試劑，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，服務生物科技領域的科學研究人員。
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