Contact us: +91 9550333722 040 - 40102781
Structured search
India
Choose your country
Different countries will display different contents
Try our best to find the right business for you.
My chemicalbook

Welcome back!

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

Related products of tetrahydrofuran

You may like

Statement: All products displayed on this website are only used for non medical purposes such as industrial applications or scientific research, and cannot be used for clinical diagnosis or treatment of humans or animals. They are not medicinal or edible.