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

GSK3179106 

Cat. No.: HY-100459 Purity: 99.40%
Handling Instructions

GSK3179106 est un inhibiteur oralement actif et sélectif de kinase RET avec des IC50s de 0,4 nM, 0,2 nM pour le RET humain et le RET du rat, respectivement. GSK3179106 a le potentiel de syndrome du côlon irritable (IBS) par l'atténuation de l'hypersensibilité viscérale post-inflammatoire et induite par le stress.

GSK3179106 ist ein oral aktiver und hochselektiver RET-Kinase-Inhibitor mit einem IC50s-Wert von 0,4 nM, 0,2 nM für die menschliche RET bzw. Ratten-RET. GSK3179106 hat das Potenzial für das Reizdarmsyndrom (IBS) durch die Dämpfung postinflammatorischer und stressbedingter viszeraler Überempfindlichkeit.

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.

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

GSK3179106 Chemical Structure

GSK3179106 Chemical Structure

CAS No. : 1627856-64-7

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10 mM * 1 mL in DMSO USD 113 In-stock
Estimated Time of Arrival: December 31
1 mg USD 50 In-stock
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5 mg USD 110 In-stock
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10 mg USD 200 In-stock
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50 mg USD 800 In-stock
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100 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
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Description

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]

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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Keywords:

GSK3179106GSK 3179106GSK-3179106RETorallyirritablebowelsyndromeIBSpost-inflammatorystress-inducedvisceralhypersensitivityInhibitorinhibitorinhibit

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