| Identification | Back Directory | [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 | [CAS]
1032754-93-0 | [Synonyms]
CS-4
RG7422
GNE 390
GDC-0980
GDC-0981
Apitolisib
GDC-0980 (RG7422)
RG7422 (Apitolisib)
Apitolisib(GDC-0980)
GDC-0980 (Apitolisib)
GDC-0980 (Apitolisib, RG7422)
Apitolisib (GDC-0980, RG7422)
GDC-0980, 98%, a potent PI3K inhibitor
GDC 0980 - RG 7422 | GNE 390 | Apitolisib
GDC-0980 (RG7422);GNE 390; GDC 0980; RG 7422
GDC-0980; RG7422; RG-7422; GDC 0980; GNE 390;GDC0980.
(S)-1-(4-((2-(2-Aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)p
(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
(2S)-1-[4-[[2-(2-AMINOPYRIMIDIN-5-YL)-7-METHYL-4-MORPHOLIN-4-YLTHIENO[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
1-Propanone, 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-, (2S)-
(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 USP/EP/BP
GNE 390
(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 GNE 390 GDC0980(RG7422) | [Molecular Formula]
C23H30N8O3S | [MDL Number]
MFCD20274520 | [MOL File]
1032754-93-0.mol | [Molecular Weight]
498.61 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
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 | [storage]
Store at -20°C | [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. |
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J & K SCIENTIFIC LTD.
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https://www.jkchemical.com |
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NCE Biomedical Co.,Ltd.
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