NVP-BSK805 2HCl (1092499-93-8(free base)) NEW
| Price | $32 | $106 | $147 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-08 |
Product Details
| Product Name: NVP-BSK805 2HCl (1092499-93-8(free base)) | Purity: 99.13% |
| Supply Ability: 10g | Release date: 2024/11/08 |
Product Introduction
Bioactivity
| 名稱 | NVP-BSK805 2HCl (1092499-93-8(free base)) |
| 描述 | NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2. |
| 細胞實驗 | 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) |
| 體外活性 | 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] |
| 體內(nèi)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] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 3 mg/mL (5.32 mM) DMSO : 113 mg/mL (200.54 mM) Ethanol : 15 mg/mL (26.62 mM) |
| 關(guān)鍵字 | NVP-BSK-805 Dihydrochloride | NVP BSK805 2HCl (1092499 93 8(free base)) | 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)) |
| 相關(guān)產(chǎn)品 | Delgocitinib | Deucravacitinib | Fedratinib | Ruxolitinib | Tofacitinib Citrate | GSK 3 Inhibitor IX | Ibrutinib | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | Tofacitinib | Gefitinib |
| 相關(guān)庫 | 抗胰腺癌化合物庫 | 經(jīng)典已知活性庫 | 表觀遺傳庫 | 激酶抑制劑庫 | 酪氨酸激酶分子庫 | 血管生成庫 | 抑制劑庫 | 抗前列腺癌化合物庫 | 已知活性化合物庫 | 抗肝癌化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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