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HomeProduct name listGSK2636771

GSK2636771

GSK2636771 Structural

What is GSK2636771?

Description

GSK2636771 is a potent, orally bioavailable, adenosine triphosphate-competitive, selective inhibitor of PI3Kβ with an apparent Ki value of 0.89 nmol/L (IC50 = 5.2 nmol/L), >900-fold selectivity over p110α and p110γ, and >10-fold selectivity over p110δ isoforms, while sparing other PI3K superfamily kinases[1-2].

The Uses of GSK2636771

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines.

in vitro

GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines. It leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines.

References

[1] Mateo, Joaquin , et al. "A first-time-in-human study of GSK2636771, a phosphoinositide 3 kinase beta-selective inhibitor, in patients with advanced solid tumors." Clinical Cancer Research (2017):clincanres.0725.2017.
[2] Sarker, Debashis , et al. "A Phase I, Open-Label, Dose-Finding Study of GSK2636771, a PI3Kβ Inhibitor, Administered with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer." Clinical Cancer Research 27.19(2021):5248-5257.

Properties of GSK2636771

Melting point: >225°C (dec.)
Boiling point: 641.3±55.0 °C(Predicted)
Density  1.38
storage temp.  -20°C Freezer
solubility  DMSO (Slightly), Methanol (Slightly)
pka -2.70±0.30(Predicted)
form  Solid
color  Pale Yellow
InChI InChI=1S/C22H22F3N3O3/c1-13-15(4-3-5-18(13)22(23,24)25)12-28-14(2)26-20-17(21(29)30)10-16(11-19(20)28)27-6-8-31-9-7-27/h3-5,10-11H,6-9,12H2,1-2H3,(H,29,30)

Safety information for GSK2636771

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for GSK2636771

InChIKey XTKLTGBKIDQGQL-UHFFFAOYSA-N
SMILES C1(C)N(CC2=CC=CC(C(F)(F)F)=C2C)C2=CC(N3CCOCC3)=CC(C(O)=O)=C2N=1

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