品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
源葉(MedMol)	S81258-5mg	99%	￥170.00元	10	-	-	-
源葉(MedMol)	S81258-10mg	99%	￥290.00元	10	-	-	-
源葉(MedMol)	S81258-50mg	99%	￥920.00元	2	-	-	-
源葉(MedMol)	S81258-100mg	99%	￥1480.00元	預(yù)計交期：2-3天	-	-	-

產(chǎn)品介紹

XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity

產(chǎn)品描述： XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity

靶點： BMK1:80 nM (Kd);BRD4:190 nM (Kd);ERK;?BMI-1;?EpigeneticReaderDomain

體外研究：
XMD8-92 (0-5 Μm; 48 hours) inhibits the proliferation of HMEC and cancer cells.
XMD8-92 effectively inhibits BMK1 activation as well as induces PML’s (promyelocytic leukemia protein) downstream effector, p21. XMD8-92 significantly inhibits basic fibroblast growth factor (bFGF) induced angiogenesis in Matrigel plugs. XMD8-92 significantly induces p21 expression in HeLa and A549 cells. Cell Viability Assay Cell Line: HMEC, A549 and HeLa cells Concentration: 0.16, 0.32, 0.63, 1.25, 2.5 or 5 μM Incubation Time: 48 hours Result: Inhibited the proliferation of HMEC and cancer cells.

體內(nèi)研究：
XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors. Animal Model: HeLa Xenograft Model (6-week-old Nod/Scid mice)[1] Dosage: 50 mg/kg Administration: I.p.; twice a day for 28 days Result: Significantly inhibited the growth of the xenografted human tumors.

參考文獻：
1. Yang Q, et al. Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.Cancer Cell. 2010 Sep 14;18(3):258-67. 2. Yang Q, et al. Targeting the BMK1 MAP kinase pathway in cancer therapy. Clin Cancer Res. 2011 Jun 1;17(11):3527-32. 3. Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016;113(42):11865-11870. 4. Umapathy G, et al. The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma. Sci Signal. 2014 Oct 28;7(349):ra102.

溶解性： soluble in DMSO

保存條件： -20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.107 ml	10.536 ml	21.072 ml
5 mM	0.421 ml	2.107 ml	4.214 ml
10 mM	0.211 ml	1.054 ml	2.107 ml
50 mM	0.042 ml	0.211 ml	0.421 ml

注意：

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XMD8-92 99%

2-[[2-ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one