1. Protein Tyrosine Kinase/RTK
  2. RET
  3. GSK3179106

GSK3179106 

製品番号: HY-100459 純度: 99.78%
取扱説明書

GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.

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GSK3179106 構造式

GSK3179106 構造式

CAS 番号 : 1627856-64-7

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 113 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 200 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 800 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1450 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

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Based on 1 publication(s) in Google Scholar

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製品説明

GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity[1].

IC50 & Target

IC50: 0.4 nM (human RET), 0.2 nM (rat RET)[1]

体外実験

GSK3179106 (10 nM-100 µM; 8 days for TT cells, 3 days for SK-N-AS and A549 cells) inhibits the proliferation of the RET-dependent TT cell line with a mean IC50 value of 25.5 nM however has no effect on the proliferation of the RET-independent SK-NAS and A549 cell lines (mean IC50>10 µM and IC30>17 µM, respectively)[1].
GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC50s of 4.6 nM and 11.1 nM, respectively[1].

Cell Viability Assay[1]

Cell Line: TT, SK-N-AS and A549 cells
Concentration: 10 nM-100 µM
Incubation Time: 8 days for TT cells, 3 days for SK-N-AS and A549 cells
Result: Inhibited the proliferation of TT cell line with a mean IC50 value of 25.5 nM however had no effect on the proliferation of the SK-NAS and A549 cell lines (mean IC50>10 µM and IC30>17 µM, respectively).
体内実験

GSK3179106 (3 or 10 mg/kg; orally; for 3.5 days BID) reduces the visceromotor response (VMR) in comparison to rats given an acetic acid enema and dosed with vehicle[1].

Animal Model: Seventy male Sprague Dawley rats (225-250 g, ~7-8 weeks old); Fifty male Fischer 344 rats (225-250 g, ~10-12 weeks old); Sprague Dawley female rats[1]
Dosage: 3 and 10 mg/kg
Administration: Oral gavage ; administered BID at 8:00 and 16:00 for 3.5 days
Result: Reduced the visceral motor response.
Led to a 34-43% inhibition in VMR to colorectal distension (CRD) at 10 mg/kg.
臨床実験
分子量

467.41

分子式

C₂₂H₂₁F₄N₃O₄

CAS 番号

1627856-64-7

SMILES

O=C(NC1=NOC(C(C)(C)C(F)(F)F)=C1)CC2=CC=C(C(C(OCC)=C3)=CNC3=O)C=C2F

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 : ≥ 100 mg/mL (213.94 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1394 mL 10.6972 mL 21.3945 mL
5 mM 0.4279 mL 2.1394 mL 4.2789 mL
10 mM 0.2139 mL 1.0697 mL 2.1394 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 (5.35 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
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Keywords:

GSK3179106GSK 3179106GSK-3179106RETorallyirritablebowelsyndromeIBSpost-inflammatorystress-inducedvisceralhypersensitivityInhibitorinhibitorinhibit

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製品名:
GSK3179106
製品番号:
HY-100459
数量:
MCE 日本正規代理店: