产品属性:
产品名称 | 规格 | CAS号 | 型号 |
ENMD-2076 | 10mM (in 1mL DMSO) 5mg 10mg 50mg 200mg | 934353-76-1 | EY-Y0165366 |
Cas No.934353-76-1
别名
化学名 6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine
分子式 C21H25N7
![ENMD-2076.png ENMD-2076.png](/SupplyImg/2022-11-29/6380532797558902231781850.jpg)
分子量 375.47
溶解度 ≥ 18.75 mg/mL in DMSO, ≥ 2.55 mg/mL in EtOH with ultrasonic
储存条件 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
产品描述:
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.
关键字: 934353-76-1;C21H25N7;ENMD-2076;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
公司具有对普通货物、冷藏及冷冻仓库的存储、包装及运输能力。
公司将始终坚持信誉立业、以人为本、质量保证、诚信服务的宗旨,不断拼搏,开拓进取,与各界朋友携手共创美好未来。