1. Protein Tyrosine Kinase/RTK
    Autophagy
  2. FLT3
    PDGFR
    Autophagy
  3. Crenolanib

Crenolanib (Synonyms: CP-868596)

製品番号: HY-13223 純度: 99.67%
取扱説明書

Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

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Crenolanib 構造式

Crenolanib 構造式

CAS 番号 : 670220-88-9

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 145 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 180 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 310 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 510 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 9 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Crenolanib purchased from MCE. Usage Cited in: bioRxiv. 2019 Jun.

    Western blots of PDGFRα and NG2 in slices treated with CP673451 and Crenolanib for 9 days.

    PDGFR アイソフォーム固有の製品をすべて表示:

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    • 参考文献

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    製品説明

    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

    IC50 & Target[1]

    PDGFRα

    2.1 nM (Kd)

    PDGFRβ

    3.2 nM (Kd)

    FLT3

    0.74 nM (Kd)

    体外実験

    Crenolanib has 25-fold more affinity for PDGFRA/B compared with KIT, and is approximately 135-fold more potent than STI571 for inhibiting the PDGFRA D842V mutation. The IC50 for crenolanib for a KIT exon 11 deletion mutant kinase is greater than 1,000 versus 8 nM for STI571. Crenolanib has low nanomolar potency against the V561D + D842V-mutant kinase that is similar to its potency against the isolated D842V mutation. Both STI571 and crenolanib potently inhibit the kinase activity of the fusion oncogene with IC50 values of 1 and 21 nM, respectively, and inhibits PDGFRA activation in this cell line with IC50 values of 93 and 26 nM, respectively[1]. HL60/VCR and K562/ABCB1 cells, overexpressing ABCB1, are 6.9- and 3.6-fold resistant to crenolanib, respectively, in relation to parental HL60 and K562 cells. PSC-833 fully reverses resistance to crenolanib in both HL60/VCR and K562/ABCB1 cells. Crenolanib (1 nM-10 μM) stimulates ABCB1 ATPase activity in a concentration-dependent manner. Crenolanib treatment does not increase the cell surface expression of ABCB1. Crenolanib inhibits [125I]-IAAP photocrosslinking of ABCB1 at high concentrations, with 50 % inhibition at 10 μM, but has little effect at lower concentrations, below 1 μM[2]. Crenolanib decreases NSCLC cell viability, induces apoptosis in NSCLC cells, and inhibits cell migration in NSCLC cells[3].

    体内実験

    Crenolanib (10 mg/kg and 20 mg/kg) suppresses non-small-cell lung cancer tumor growth in vivo and induces tumor cell apoptosis, and the dosage of crenolanib applied is well tolerated by recipient mice[3].

    臨床実験
    分子量

    443.54

    分子式

    C₂₆H₂₉N₅O₂

    CAS 番号

    670220-88-9

    SMILES

    NC1CCN(C2=CC=CC3=C2N=C(N4C5=CC=C(C=C5N=C4)OCC6(COC6)C)C=C3)CC1

    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 : 33.33 mg/mL (75.15 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2546 mL 11.2729 mL 22.5459 mL
    5 mM 0.4509 mL 2.2546 mL 4.5092 mL
    10 mM 0.2255 mL 1.1273 mL 2.2546 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: ≥ 3 mg/mL (6.76 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 3 mg/mL (6.76 mM); Clear solution

    • 3.

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

      Solubility: ≥ 3 mg/mL (6.76 mM); Clear solution

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

    Viable cell numbers following drug treatment are measured using the WST-1 assay. Briefly, 1×103 cells are seeded in 100 μL complete medium per well in 96-well tissue culture plates and incubated with crenolanib (0-10 μM) at 37°C in 5% CO2 for 96 h. 10 μL WST-1 reagent is then added to each well, incubation is continued for two additional hours and the color developed is quantified according to the manufacturer’s instructions. Each experiment is performed in triplicate. IC50 concentrations are calculated by the least square fit of dose–response inhibition in a non-linear regression model using GraphPad Prism V software.

    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
    [3]

    A549 cells are injected into the axillary regions of mice (2×106 cells/mouse). When the tumor volumes reached 70 mm3, the mice are randomLy allocated to the control group, low-dose crenolanib group (10 mg/kg), or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight are measured every other day for about 2 weeks. The tumor volume is calculated as follows: (mm3)=(width×width×length)/2. After treatment, the mice are euthanized using carbon dioxide, and the tumors are harvested and analyzed.

    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
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    Keywords:

    CrenolanibCP-868596CP868596CP 868596FLT3PDGFRAutophagyCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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    製品名:
    Crenolanib
    製品番号:
    HY-13223
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