化合物NVP-BSK805 2HCl T6294

Product Introduction
Bioactivity


英文名: NVP-BSK805 2HCl (1092499-93-8(free base))

描述: NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805) 是一种特异性有效的 ATP 竞争性 JAK2 抑制剂，其特异性是 JAK1、JAK3 和 TYK2 的 20 倍以上。

细胞实验: The anti-proliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours with an 8-point concentration range of compound and cell proliferation relative to DMSO-treated cells is measured using the colorimetric WST-1 (Roche Diagnostics GmbH) cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 (ID Business Solutions, Ltd.) to determine the half-maximal growth inhibition (GI50) values.(Only for Reference)

体外活性: NVP-BSK805 is found to potently inhibit JAK2, whereas displaying more than 20-fold selectivity towards JAK1, JAK3, and TYK2. NVP-BSK805 causes half-maximal inhibition of full-length JAK2V617F and JAK2 wild-type enzymes at 0.5 nM. NVP-BSK805 blocks the growth of JAK2V617F cells (Ba/F3) and induces apoptosis with a GI50 at concentrations ＜100 nM. As constitutive STAT5 phosphorylation in dependent on JAK2, NVP-BSK805 is found to potently suppress STAT5 phophorylation at ≥ 100 nM concentrations in the JAK2 V617F -mutant cell lines, like MB-02. Incubation of SET-2 cells with 150 nM and 1 μM of NVP-BSK805, which corresponds to concentration yielding 75% and 95% growth inhibition, respectively, for 24, 48, and 72 hours lead to concentration- and time- dependent induction of apoptosis. These results are evidenced by the detection of cleaved PARP, reduced Bcl-xL expression, and a strong increase in the number of cells with less than 2N DNA content. [1] NVP-BSK805 triggered cell death requires activation of caspase cascades and is overcome by caspase inhibition in both SET-2 and MB-02 cells. NVP-BSK805 modulates the post-translational modification of Bim and levels of Mcl-1 in JAK2V617F cells, SET-2 and MB-02 cells. [2]

体内活性: Oral bioavailability of NVP-BSK805 in mice is estimated to be 45%, while it is 50% in rats. Oral administration of NVP-BSK805 at 150 mg/kg suppresses STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell–driven mouse model. NVP-BSK805 suppresses rhEpo-induced STAT5 phosphorylation as well as rhEpo-mediated polycythemia and splenomegaly in BALB/c mice at doses of 25, 50, and 100 mg/kg orally. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 3 mg/mL (5.32 mM)
DMSO : 113 mg/mL (200.54 mM)
Ethanol : 15 mg/mL (26.62 mM)


关键字: NVP-BSK-805 Dihydrochloride | NVP BSK805 2HCl (1092499 93 8(free base)) | BSK805 | 盐酸NVP-BSK805 | NVP-BSK-805 | NVPBSK805 2HCl (1092499938(free base)) | NVP-BSK 805 Dihydrochloride | NVP-BSK 805 | NVP-BSK805 Dihydrochloride | NVP-BSK805 2HCl (1092499-93-8 free base) | NVP-BSK805 | BSK-805 | NVP-BSK805 2HCl (1092499-93-8(free base)) | NVP-BSK-805 2HCl (1092499-93-8(free base))

相关产品: Pacritinib | Tafetinib | Vamotinib | Vidarabine | NVP-AEW541 | Ibrutinib | ST271 | GSK 3 Inhibitor IX | GLPG0634 analog | Larotinib

相关库: Anti-Prostate Cancer Compound Library | Anti-Cancer Compound Library | Angiogenesis related Compound Library | Anti-Lung Cancer Compound Library | Kinase Inhibitor Library | Inhibitor Library | Epigenetics Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途