GDC-0941 | pan-PI3K inhibitor

CAS:
957054-30-7
Catalog Number:
10-2141
Activity:
pan-Class I PI3-kinase inhibitor
Chemical Names:
4-[2-(1H-Indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine; Pictilisib
Molecular Weight:
513.64
Molecular Formula:
C23H27N7O3S2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White/off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
5 mg$58.00
25 mg$160.00

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

References/Citations:

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

CAS:
957054-30-7
Catalog Number:
10-2141
Activity:
pan-Class I PI3-kinase inhibitor
Chemical Names:
4-[2-(1H-Indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine; Pictilisib
Molecular Weight:
513.64
Molecular Formula:
C23H27N7O3S2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White/off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee