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HomeProduct name listGDC-0068

GDC-0068

GDC-0068 Structural

What is GDC-0068?

The Uses of GDC-0068

GDC-0068 is a highly selective AKT inhibitor targeting Akt1 , Akt2 and Akt3. Studies have shown its use in combination with vemurafenib (V118500), have demonstrated therapeutic value in the treatment of hyperproliferative disorders such as cancer.

The Uses of GDC-0068

DC-0068 is a highly selective pan-Akt inhibitor targeting Akt1, Akt2, and Akt3 with IC50 of 5 nM, 18 nM, and 8 nM, respectively.

The Uses of GDC-0068

(2S)-2-(4-Chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone is a highly selective AKT inhibitor targeting Akt1, Akt2 and Akt3. Studies have shown its use in combination with vemurafenib (V118500), have demonstrated therapeutic value in the treatment of hyperproliferative disorders such as cancer.

Definition

ChEBI: (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone is a N-arylpiperazine.

Biological Activity

gdc-0068 (rg7440) is a highly selective small molecule inhibitor of akt with ic50s of 5, 18 and 8 nm for akt1, akt2 and akt3. the pi3k-akt pathway regulates cell growth, survival and tumorigenesis. gdc-0068 binds to and blocks the activation of akt, which result in cell cycle arrest, inhibition of tumor cell proliferation and induction of tumor cell death. pi3k-akt is pathway frequently activated in tumors, thus tumors with pten or pi3k mutations, which lead to activation of akt are with high sensitivity to gdc-0068. gdc-0068 is now used for the treatment of human cancers.1. discovery and preclinical pharmacology of a selective atp-competitive akt inhibitor (gdc-0068) for the treatment of human tumors. jf blake, r xu, jr bencsik, d xiao… - journal of medicinal 20122. lin j, sampath d, nannini ma, et al: targeting activated akt with gdc-0068, a novel selective akt inhibitor that is efficacious in multiple tumor models. clin canc res 2013, 19:1760–1772.

Properties of GDC-0068

Melting point: >106°C (dec.)
Boiling point: 669.4±55.0 °C(Predicted)
Density  1.254
storage temp.  Hygroscopic, Refrigerator, under inert atmosphere
solubility  Soluble in DMSO.
pka 13.11±0.40(Predicted)
form  Solid
color  Peach

Safety information for GDC-0068

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.
P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405:Store locked up.

Computed Descriptors for GDC-0068

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