(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 NO.:1032754-93-0
- Empirical Formula: C23H30N8O3S
- Molecular Weight: 498.6
- MDL number: MFCD20274520
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-17 16:00:36
What is (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?
The Uses of (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
GDC-0980 is used in the synthesis of PI3K inhibitors to treat carcinomas. Potent PI3K/mTOR dual Inhibitor.
What are the applications of Application
GDC-0980 is a PI3K and FRAP (mTOR) kinase 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].
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.
Properties of (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
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 |
Safety information for (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
Computed Descriptors for (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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