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| | Pictilisib Basic information |
| Product Name: | Pictilisib | | Synonyms: | Pictilisib;Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-;GDC-0941;GDC-0941 free base;2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine;GDC-0941 bismesylate;2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine;4-(2-(1H-Indazol-4-yl)-6-((4-(Methylsulfonyl)piperazin-1-yl)Methyl)thieno[3,2-d] | | CAS: | 957054-30-7 | | MF: | C23H27N7O3S2 | | MW: | 513.64 | | EINECS: | 1312995-182-4 | | Product Categories: | An inhibitor of class I PI3 kinase (PI3K).;Inhibitors;Akt;mTOR;PI3K | | Mol File: | 957054-30-7.mol |  |
| | Pictilisib Chemical Properties |
| Melting point | >200oC (dec.) | | density | 1.53±0.1 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (>25 mg/ml) | | form | White powder solid. | | pka | 12.22±0.40(Predicted) | | color | White/off-white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| | Pictilisib Usage And Synthesis |
| Description | GDC-0941/Pictilisib (957054-30-7) is a potent and selective inhibitor of class I phosphatidylinositol-3-kinases (PI3K) with significant antitumor activity – IC50’s: PI3Kα = 3nM, PI3Kβ = 33 nM, PI3Kδ = 3 nM, PI3Kγ = 75 nM.1,2?? GDC-0941 is the chemical probe of choice for the pan-inhibition of class I PI3K’s.3?Currently in clinical trials.4 | | Uses | GDC-0941 is a potent and selective oral inhibitor of the class I PI3K. GDC-0941 demonstrated broad spectrum of activity in breast, ovarian, lung, and prostate cancer models. Studies has also shown GDC-0941 may enhance anti-tumor activity of Docetaxel (D494420) in human breast cancer models. Potent PI3K inhibitor. | | Uses | GDC-0941 is a potent and selective oral inhibitor of the class I PI3K. GDC-0941 demonstrated broad spectrum of activity in breast, ovarian, lung, and prostate cancer models. Studies has also shown GDC
-0941 may enhance anti-tumor activity of Docetaxel (D494420) in human breast cancer models. | | Definition | ChEBI: A sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. | | target | PI3Kα | | References | 1) Folkes?et al.?(2008),?The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine(GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer;? J.?Med. Chem.,?51?5522
2) Raynaud?et al. (2009),?Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinase: from PI-103 through PI-540, PI620 to the oral agent GDC-0941; Mol. Cancer Ther.,?8?1725
3) Knapp et al. (2013),?A public-private partnership to unlock the untargeted kinome; Nat. Chem. Biol.,?9?3
4) Sarker?et al. (2015),?First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors; Clin. Cancer Res.,?21?77 |
| | Pictilisib Preparation Products And Raw materials |
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