GSK2606414_DataSheet_MedChemExpress
Inhibitors, Agonists, Screening Libraries
https://www.wendangku.net/doc/1914293149.html, Data Sheet
BIOLOGICAL ACTIVITY:
GSK2606414 is an orally available and selective PERK inhibitor with an IC 50 of 0.4 nM.
IC50 & Target: IC50: 0.4 nM (PERK)
In Vitro: GSK2606414 inhibits PERK activation in cells [1].
In Vivo: GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice [1].
PROTOCOL (Extracted from published papers and Only for reference)
Animal Administration: GSK2606414 is formulated in vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in
water, pH 4.8).[1]Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with –200 mm 3 tumors are randomized into various treatment groups (n = 8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in
water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated using the following equation: tumor volume (mm 3) = (length × width 2)/2. Results are represented as percent inhibition on completion of dosing, which is 100[1–(average growth of drug–treated population)/(average growth of vehicle–treated control population)]. Statistical analysis is performed using a two–tailed t test.
References:
[1]. Axten JM, et al. Discovery of 7–methyl–5–(1–<[3–(trifluoromethyl)phenyl]acetyl>–2,3–dihydro–1H–indol–5–yl)–7H–pyrrolo[2,3–d]pyrimidin–4–amine (GSK2606414), a potent and selective first–in–class inhibitor of protein kinase R (PKR)–like endoplasmic reticulu
Product Name:
GSK2606414Cat. No.:
HY-18072CAS No.:
1337531-36-8Molecular Formula:
C 24H 20F 3N 5O Molecular Weight:
451.44Target:
PERK Pathway:
Cell Cycle/DNA Damage Solubility:
DMSO: ≥ 31 mg/mL
Caution: Product has not been fully validated for medical applications. For research use only.
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https://www.wendangku.net/doc/1914293149.html,