GDC-0068

Bezeichnung:GDC-0068

CAS-Nr1001264-89-6

Englisch Name:GDC-0068

CBNumberCB52627897

SummenformelC24H32ClN5O2

Molgewicht458

MOL-Datei1001264-89-6.mol

GDC-0068 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>106°C (dec.)
Siedepunkt	669.4±55.0 °C(Predicted)
Dichte	1.254
storage temp.	Hygroscopic, Refrigerator, under inert atmosphere
Löslichkeit	Soluble in DMSO.
pka	13.11±0.40(Predicted)
Aggregatzustand	Solid
Farbe	peachy

Gefahreninformationscode (GHS)

GDC-0068 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
(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.
Verwenden
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.
Verwenden
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.
Biologische Aktivität
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-0068 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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