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GDC-0068

GDC-0068 Structure
GDC-0068
  • CAS No.1001264-89-6
  • Chemical Name:GDC-0068
  • CBNumber:CB52627897
  • Molecular Formula:C24H32ClN5O2
  • Formula Weight:458
  • MOL File:1001264-89-6.mol
GDC-0068 Property
  • 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
  • FDA UNII 524Y3IB4HQ
  • NCI Drug Dictionary ipatasertib
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P280a-P304+P340-P305+P351+P338-P405-P501a

GDC-0068 Chemical Properties,Usage,Production

  • 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 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)
GDC-0068 Preparation Products And Raw materials
Raw materials
Preparation Products
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GDC-0068 Spectrum
1001264-89-6, GDC-0068Related Search:
  • PI3K/Akt/mTOR
  • Inhibitor
  • Inhibitors
  • PI3K
  • mTOR
  • Akt
  • 信号转导通路激酶抑制剂
  • 抑制剂
  • 药靶配体
  • 合成有机化合物配体
  • 精细化工产品
  • 细胞生物学试剂
  • 小分子抑制剂,天然产物
  • C24H32ClN5O2
  • 1002364-89-6
  • GDC-0068(IPATASERTIB,RG7440,GDC0068) |CAS 1001264-89-6
  • 帕他色替,10 MM DMSO 溶液
  • GDC-0068,帕他色替
  • (S)-2-(4-氯苯基)-1-(4-((5R,7R)-7-羟基-5-甲基-6,7-二氢-5H-环戊并[D]嘧啶-4-基)哌嗪-1-基)-3-(异丙胺基)丙-1-酮
  • GDC-0068|||RG7440|||帕他色替
  • GDC-0068,AKT1 / 2/3抑制剂
  • (2S)-2-(4-氯苯基)-1-[4-[(5R,7R)-6,7-二氢-7-羟基-5-甲基-5H-环
  • (S)-2-(4-氯苯基)-1-(4-((5R,7R)-7-羟基-5-甲基-6,7-二氢-5H-环戊基[D]嘧啶-4-基)哌嗪-1-基)-3-(异丙胺基)丙-1-酮
  • IPATASERTIB(GDC-0068)帕他色替
  • IPATASERTIB 二盐酸盐
  • IPATASERTIB,帕他色替
  • GDC-0068, 一种选择性的 PAN-AKT 抑制剂
  • AKT广谱抑制剂(GDC-0068)
  • 帕他色替
  • (2S)-2-(4-氯苯基)-1-[4-[(5R,7R)-6,7-二氢-7-羟基-5-甲基-5H-环戊并嘧啶-4-基]-1-哌嗪基]-3-[(1-甲基乙基)氨基]-1-丙酮
  • 盐酸盐GDC-0068
  • 1001264-89-6
  • Ipatasertib, 10 mM in DMSO
  • GDC-0068 Ipatasertib RG-7440 GDC0068 RG7440
  • Cenicriviroc mesylate
  • Ipatasertib
  • GDC-0068 (Ipatasertib,RG-7440)
  • GDC0068;GDC 0068;GDC-0068
  • CS-543
  • GDC-0068, 98%, a highly selective pan-Akt inhibitor
  • EOS-62198
  • GDC0068;GDC 0068;GDC-0068;RG7440;RG-7440;;RG 7440
  • patasertib
  • GDC-0068 USP/EP/BP
  • 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)-
  • RG7440
  • GDC-0068(RG7440)
  • GDC-0068
  • (S)-2-(4-Chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-
  • GDC-0068 (Ipatasertib)
  • GDC-0068;RG7440; GDC0068; GDC 0068; RG-7440; RG 7440
  • Ipatasertib (GDC-0068,RG 7440)
  • (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
  • 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
  • (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)
  • (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
  • Ipatasertib (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