1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. BMS-911543

BMS-911543 

製品番号: HY-15270 純度: 97.80%
取扱説明書

BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).

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BMS-911543 構造式

BMS-911543 構造式

CAS 番号 : 1271022-90-2

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 126 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 84 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 132 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 228 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 840 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1320 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

    BMS-911543 purchased from MCE. Usage Cited in: IUBMB Life. 2018 Jan;70(1):81-91.

    A549 cells are treated with TG101348 (3 nM), BMS-911543 (1.5 nM), and Stattic (2.5 lM) for 24 h, and the conditioned media are collected and applied for tube formation assay in HUVECs.

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    製品説明

    BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).

    IC50 & Target[1]

    JAK2

    1.1 nM (IC50)

    Tyk2

    66 nM (IC50)

    JAK1

    75 nM (IC50)

    JAK3

    360 nM (IC50)

    体外実験

    BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively). BMS-911543 displays IC50 of >25 μM for all targets except PDE4 (IC50, 5.6 μM). BMS-911543 exhibits potent antiproliferative effect on the SET-2 and BaF3-V617F engineered cell lines (both dependent upon JAK2 pathway), with IC50s of 60 and 70 nM, respectively, and such an effect on SET-2 and BaF3-V617F cells is correlated with similar activity on constitutively active pSTAT5 (IC50, 80 and 65 nM, respectively)[1]. BMS-911543 (>20 μM) is cytotoxic to murine or human pancreatic ductal adenocarcinoma (PDAC) cell lines. BMS-911543 (5 and 10 μM) also blocks T regulatory cell differentiation in vitro[2].

    体内実験

    BMS-911543 is well tolerated up to 100 mg/kg in rats (mean AUC0-72 h, 11300 μM·h) and dogs (AUC0-24 h, 610 μM·h). A 15 mg/kg/day dose (Day 14 AUC0-24 h, 3200 μM·h) is well tolerated[1] in two-week repeat dose studies in rats. BMS-911543 (30 mg/kg, p.o.) suppresses the growth of tumor and prolongs the median survival in KPC-Brca1 mice. BMS-911543 also selectively reduces pSTAT5 expression in pancreatic tumors and decreases levels of intratumoral FoxP3+ T regulatory cells in mice administered BMS-911543[2].

    臨床実験
    分子量

    432.52

    分子式

    C₂₃H₂₈N₈O

    CAS 番号

    1271022-90-2

    SMILES

    O=C(C1=CC2=C(N(C)C=N3)C3=C(NC4=NN(C)C(C)=C4)N=C2N1CC)N(C5CC5)C6CC6

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 25 mg/mL (57.80 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3120 mL 11.5602 mL 23.1203 mL
    5 mM 0.4624 mL 2.3120 mL 4.6241 mL
    10 mM 0.2312 mL 1.1560 mL 2.3120 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献
    細胞実験
    [2]

    Human and murine pancreatic ductal adenocarcinoma (PDAC) tumor cells or PSC are cultured in 96 well plates and the following day treated with BMS-911543 or DMSO vehicle control for 48 hours. After 48 hours, MTT reagent (ATCC) is added for 2 hours at 37°C. Samples are analyzed on a plate reader testing for absorbance at 450 nM[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [2]

    Mice[2]
    Pancreatic tumors are confirmed in KPC-Brca1 mice by bioluminescent imaging (BLI) at 5-6 weeks of age. Briefly, mice are maintained on isofluorane anesthesia and imaged 10-15 minutes following intraperitoneal injection of Luciferin on a heated platform. Animals with a pancreatic mass of approximately 50-100 mm3 are randomized, and treatment is initiated the day following imaging. Mice are then treated for 2 weeks by daily oral gavage at a dose of 30 mg/kg BMS-911543. Following 2 weeks of treatment, animals are euthanized via CO2 asphyxiation followed by cardiac puncture. Plasma, splenocytes and tumor tissue are collected for further analysis. Pathology is assessed by H&E to determine differentiation state of the tissue as PanIN, papillary carcincoma or PDAC. For long term in vivo experiments, 8 week old KPC-Brca1 mice with advanced disease are continuously treated by oral gavage at 30 mg/kg of BMS-911543 until mice meet specified early removal criteria[2].

    MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    純度: 97.80%

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    Keywords:

    BMS-911543BMS911543BMS 911543JAKJanus kinaseInhibitorinhibitorinhibit

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    製品名:
    BMS-911543
    製品番号:
    HY-15270
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