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ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  PI3K / Akt / mTOR >  PI3K inhibitor >  (S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one

(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one

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(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one Basic information

Product Name:
(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one
Synonyms:
  • (S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one
  • GNE 390
  • GDC-0980
  • (S)-1-(4-((2-(2-aMinopyriMidin-5-yl)-7-Methyl-4-Morpholinothieno[3,2-d]pyriMidin-6-yl)Methyl)piperazin-1-yl)-2-hydroxypropan-1-one
  • GDC-0980 (RG7422)
  • RG7422
  • Apitolisib
  • Apitolisib (GDC-0980, RG7422)
CAS:
1032754-93-0
MF:
C23H30N8O3S
MW:
498.6
Product Categories:
  • Akt
  • mTOR
  • PI3K
  • Inhibitors
  • PI3K/Akt/mTOR
  • An inhibitor of Class I PI3 kinase and mTOR kinase.
Mol File:
1032754-93-0.mol
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(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one Chemical Properties

Melting point:
>202°C (dec.)
Density 
1.399
storage temp. 
-20°C Freezer
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form 
Solid
pka
13.90±0.20(Predicted)
color 
White to Light Yellow
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(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one Usage And Synthesis

Uses

GDC-0980 is used in the synthesis of PI3K inhibitors to treat carcinomas. Potent PI3K/mTOR dual Inhibitor.

Biological Activity

gdc-0980 (rg7422) is a selective, novel, potent and orally bioavailable inhibitor of class 1 pi3k/mtor kinase with the ki value of 17nmol/l for mtor kinase [1].gdc-0980 (rg7422) has shown the effective inhibition with the ic50 values of ＜200nmol/l in prostate, breast and nsclc lines, respectinely. in addition, gdc-0980 (rg7422) has been reported to reduce cell viability in kpl4 cells by cell-cycle inhibition and induction of apoptosis with the ic50 value of 109nm and the ec50 value of 78nm. furthermore, gdc-0980 (rg7422) has been revealed to significantly inhibit tumor responses in xenograft models in oral dose of the compound. besides, gdc-0980 (rg7422) has been noted to enhance the antitumor activity in combination with antitumor agents ( docetaxel) in vivo [1].

Synthesis

1032757-58-6

1173206-16-0

1032754-93-0

The reaction was carried out according to general procedure B using HCl salt of 2-chloro-7-methyl-4-morpholino-6-((piperazin-1-yl)methyl)thieno[3,2-d]pyrimidine (590 mg) and lactic acid to synthesize (S)-1-(4-((2-chloro-7-methyl-4-morpholino-thieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2- hydroxypropan-1-one.

in vivo

Apitolisib (GDC-0980) (1 mg/kg, p.o.) demonstrats significant efficacy in mouse xenografts and is currently in phase I clinical trials for cancer. Clearance and PPB are low, and Apitolisib (GDC-0980) shows dose-proportional exposure from 5 mg/kg dosed in PEG to 50 mg/kg dosed in suspension in MCT, a finding attributed partially to the compound’s good solubility[1]. Apitolisib (GDC-0980) (5 mg/kg, p.o.) results in greater than 50% TGI in 15 of the 20 xenograft models. The difference in tumor response to Apitolisib (GDC-0980) treatment correlates with the duration of knockdown of pAkt/tAkt[2].

target

p110α

IC 50

PI3Kα: 5 nM (IC50); PI3Kδ: 7 nM (IC50); PI3Kγ: 14 nM (IC50); PI3Kβ: 27 nM (IC50); mTOR: 17 nM (Ki); TORC1; TORC2

References

[1] wallin jj1, edgar ka, guan j, berry m, prior ww, lee l, lesnick jd, lewis c, nonomiya j, pang j, salphati l, olivero ag, sutherlin dp, o'brien c, spoerke jm, patel s, lensun l, kassees r, ross l, lackner mr, sampath d, belvin m, friedman ls. gdc-0980 is a novel class i pi3k/mtor kinase inhibitor with robust activity in cancer models driven by the pi3k pathway. mol cancer ther. 2011 dec;10(12):2426-36. doi: 10.1158/1535-7163.mct-11-0446. epub 2011 oct 13.

(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-oneSupplier

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(S)-1-[4-[[2-(2-Aminopyrimidin-5-yl)-7-methyl-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]methyl]piperazin-1-yl]-2-hydroxypropan-1-one(1032754-93-0)Related Product Information