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GSK3179106 

Cat. No.: HY-100459 Purity: 99.78%
Handling Instructions

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM.

For research use only. We do not sell to patients.

GSK3179106 Chemical Structure

GSK3179106 Chemical Structure

CAS No. : 1627856-64-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 555 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 540 In-stock
Estimated Time of Arrival: December 31
10 mg USD 900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3960 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM[1].

IC50 & Target

IC50: 0.4±0.2 nM (Human RET), 0.2±0.1 nM (Rat RET)[1]

In Vitro

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).
In Vivo

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.
Clinical Trial
Molecular Weight

467.41

Formula

C₂₂H₂₁F₄N₃O₄

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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.
In Vivo:
  • 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.
References
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GSK3179106
Cat. No.:
HY-100459
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