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  2. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  3. JAK
  4. NVP-BSK805

NVP-BSK805 是一種 ATP 競爭性的 JAK2 抑制劑，對 JAK2 JH1 (JAK 同源 1)，JAK1 JH1，JAK3 JH1，和 TYK2 JH1 的 IC50 值分別為 0.48 nM，31.63 nM，18.68 nM 和 10.76 nM。

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NVP-BSK805 Chemical Structure

NVP-BSK805 Chemical Structure

CAS No. : 1092499-93-8

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1727
In-stock
1 mg ￥609
In-stock
5 mg ￥1600
In-stock
10 mg ￥2600
In-stock
25 mg ￥5200
In-stock
50 mg 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

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Other Forms of NVP-BSK805:

查看 JAK 亞型特異性產品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

生物活性

NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].

IC50 & Target[1]

JAK2 JH1

0.48 nM (IC50)

FL JAK2 V617F

0.56 nM (IC50)

FL JAK2 wt

0.58 nM (IC50)

TYK2 JH1

10.76 nM (IC50)

JAK3 JH1

18.68 nM (IC50)

JAK1 JH1

31.63 nM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
SET-2 GI50
88 nM
Compound: 26
Growth inhibition of human SET2 cells expressing JAK2V617F mutant after 72 hrs by colorimetric WST1 assay
Growth inhibition of human SET2 cells expressing JAK2V617F mutant after 72 hrs by colorimetric WST1 assay
[PMID: 20231096]
體外研究
(In Vitro)

NVP-BSK805 (BSK 805) is a JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC50s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated Ki of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2V617F-bearing acute myeloid leukemia cell lines with GI50 of <100 nM. NVP-BSK805 blocks the STAT5 phosphorylation at ≥100 nM concentrations, and shows a bias for JAK2 over JAK1 and JAK3 inhibition in the JAK2V617F-mutant cell lines[1].
NVP-BSK805 (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內研究
(In Vivo)

NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

490.55

Formula

C27H28F2N6O
CAS 號
性狀

固體

顏色

Off-white to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (203.85 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 2.0385 mL 10.1926 mL 20.3853 mL
5 mM 0.4077 mL 2.0385 mL 4.0771 mL
查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料

純度: 99.89%

參考文獻
Cell Assay
[1]

The antiproliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours (96 hours for MB-02 and MUTZ-8 cells) with an 8-point concentration range of NVP-BSK805 and cell proliferation relative to NVP-BSK805 is measured using the colorimetric WST-1 cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 to determine the half-maximal growth inhibition (GI50) values[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Concomitantly with NVP-BSK805 treatment, female BALB/c mice receive daily s.c. injections (in 100 μL saline buffer) of 10 units of rhEpo for 4 consecutive days. Controls are injected corresponding volumes of saline buffer. Mice are sacrificed 24 hours after the final dose and total blood, spleen, and bone marrow are taken for further analysis. Animals are 8 to 10 weeks of age at treatment start (20-25 g body weight) and are kept under optimal hygienic conditions with free access to food and water[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻

完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內使用，-20°C儲存時，請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0385 mL 10.1926 mL 20.3853 mL 50.9632 mL
5 mM 0.4077 mL 2.0385 mL 4.0771 mL 10.1926 mL
10 mM 0.2039 mL 1.0193 mL 2.0385 mL 5.0963 mL
15 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3975 mL
20 mM 0.1019 mL 0.5096 mL 1.0193 mL 2.5482 mL
25 mM 0.0815 mL 0.4077 mL 0.8154 mL 2.0385 mL
30 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
40 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2741 mL
50 mM 0.0408 mL 0.2039 mL 0.4077 mL 1.0193 mL
60 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
80 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6370 mL
100 mM 0.0204 mL 0.1019 mL 0.2039 mL 0.5096 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產品名稱：
NVP-BSK805
目錄號：
HY-14722
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