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GSK3179106

Cat. No. M10933

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GSK3179106  Structure
Size Price Availability Quantity
5mg USD 115 In stock
10mg USD 200 In stock
25mg USD 400 In stock
50mg USD 700 In stock
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Quality Control & Documentation
Biological Activity

GSK3179106 is an orally active, selective RET kinase inhibitor for human and rat RET IC50 0.4 nM and 0.2 nM, respectively. GSK3179106 has the potential for use in irritable bowel syndrome (IBS) by reducing post-inflammatory and stress-induced visceral hypersensitivity reactions.

Chemical Information
Molecular Weight 467.41
Formula C22H21F4N3O4
CAS Number 1627856-64-7
Form Solid
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Joanne E Kearon, et al. Mol Cell Neurosci. GDNF requires HIF-1α and RET activation for suppression of programmed cell death of enteric neurons by metabolic challenge

[2] John P Russell, et al. J Pharmacol Exp Ther. Exploring the Potential of RET Kinase Inhibition for Irritable Bowel Syndrome: A Preclinical Investigation in Rodent Models of Colonic Hypersensitivity

[3] John P Russell, et al. Neurogastroenterol Motil. Enteric RET inhibition attenuates gastrointestinal secretion and motility via cholinergic signaling in rat colonic mucosal preparations

[4] Melisa Cooper, et al. Clin Pharmacol Drug Dev. First-in-Human Studies for a Selective RET Tyrosine Kinase Inhibitor, GSK3179106, to Investigate the Safety, Tolerability, and Pharmacokinetics in Healthy Volunteers

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Keywords: GSK3179106 supplier, RET, inhibitors, activators

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