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GDC-0068

Basic information Safety Supplier Related

GDC-0068 Basic information

Product Name:
GDC-0068
Synonyms:
  • GDC-0068
  • GDC-0068(RG7440)
  • RG7440
  • (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
  • Ipatasertib (GDC-0068)
  • GDC0068;GDC 0068;GDC-0068;RG7440;RG-7440;;RG 7440
  • Ipatasertib
  • (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
CAS:
1001264-89-6
MF:
C24H32ClN5O2
MW:
458
Product Categories:
  • Akt
  • mTOR
  • Inhibitor
  • PI3K/Akt/mTOR
  • Inhibitors
  • PI3K
Mol File:
1001264-89-6.mol
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GDC-0068 Chemical Properties

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 
peachy
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GDC-0068 Usage And Synthesis

Uses

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.

Uses

(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.

Uses

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.

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.

target

Akt1

GDC-0068Supplier

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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jkinfo@jkchemical.com
Chembest Research Laboratories Limited
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021-20908456
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sales@BioChemBest.com
JinYan Chemicals(ShangHai) Co.,Ltd.
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13817811078
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sales@jingyan-chemical.com
Jinan Trio PharmaTech Co., Ltd.
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+86 (531) 88811783
Email
sales@trio-pharmatech.com (International market)