| Identification | Back Directory | [Name]
GDC-0068 | [CAS]
1001264-89-6 | [Synonyms]
RG7440
CS-543
GDC-0068
EOS-62198
patasertib
Ipatasertib
GDC-0068(RG7440)
GDC-0068 USP/EP/BP
Cenicriviroc mesylate
GDC-0068 (Ipatasertib)
Ipatasertib (GDC-0068)
GDC0068;GDC 0068;GDC-0068
GDC-0068 (Ipatasertib,RG-7440)
Ipatasertib (GDC-0068,RG 7440)
GDC0068;GDC 0068;GDC-0068;RG7440;RG-7440;;RG 7440
GDC-0068, 98%, a highly selective pan-Akt inhibitor
GDC-0068;RG7440; GDC0068; GDC 0068; RG-7440; RG 7440
(S)-2-(4-Chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-
(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
(2S)-2-(4-Chlorophenyl)-1-{4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl}-3-(isopropylamino)-1-propanone
(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
1-Propanone, 2-(4-chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-, (2S)-
(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)
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 | [Molecular Formula]
C24H32ClN5O2 | [MDL Number]
MFCD22124514 | [MOL File]
1001264-89-6.mol | [Molecular Weight]
458 |
| Chemical Properties | Back Directory | [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. | [form ]
Solid | [pka]
13.11±0.40(Predicted) | [color ]
peachy |
| Hazard Information | Back Directory | [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]
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. | [in vivo]
Ipatasertib (30 mg/kg; p.o.; single daily for 15 consecutive days) exhibits PUMA-dependent antitumor activity in HCT116 WT and PUMA?/? cells xenograft nude mice model[1]. | Animal Model: | HCT116 WT and PUMA?/? cells xenograft nude mice model[1]. | | Dosage: | 30 mg/kg | | Administration: | Oral gavage; single daily for 15 consecutive days. | | Result: | Inhibited growth of tumors in a PUMA-dependent manner. |
| [target]
Akt1 | [IC 50]
Akt1: 5 nM (IC50); Akt3: 8 nM (IC50); Akt2: 18 nM (IC50); PKA: 3100 nM (IC50) |
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