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Pictilisib

Pictilisib structure

CAS No:
957054-30-7
Formula:
C23H27N7O3S2
Chemical Name:
Pictilisib
Synonyms:
Thieno[3,2-d]pyrimidine,2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-;2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine;4-[2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)piperazin-1-yl]methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine;GDC 0941;Pictilisib;GDC 941;GNE 0941;1146702-55-7
Categories:
Biochemical Engineering > Inhibitors

Description

GDC-0941 (Pictilisib) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

Pictrelisib is a sulfonamide composed of indazole, morpholine, and methylsulfonyl-substituted piperazine rings bound to a thienopyrimidine ring. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor. It is a sulfonamide, a member of piperazines, a member of morpholines, a member of indazoles and a thienopyrimidine.|Pictilisib has been used in trials studying the treatment of Solid Cancers, Breast Cancer, Advanced Solid Tumours, Metastatic Breast Cancer, and Non-Hodgkin's Lymphoma, Solid Cancers, among others.|Pictilisib is a small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K), with potential antineoplastic activity. Upon administration, pictilisib selectively binds to PI3K in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway. This may result in inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis; dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Pictilisib Basic Attributes

Molecular Weight：

513.64

Exact Mass：

513.64

EC Number：

1312995-182-4

UNII：

ICY00EMP8P

DSSTox ID：

DTXSID40241930

NCI Thesaurus Code：

C165479

HScode：

29350090

Characteristics

PSA：

144

XLogP3：

1.6

Density：

1.5±0.1 g/cm3

Flash Point：

369.7±34.3 °C

Refractive Index：

1.753

Drug Information

MeSH Entry Terms：

2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine

Pictilisib Use and Manufacturing

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.

Computed Properties

Molecular Weight:513.6
XLogP3:1.6
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:5
Exact Mass:513.16168010
Monoisotopic Mass:513.16168010
Topological Polar Surface Area:144
Heavy Atom Count:35
Complexity:832
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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