GDC0941 - CAS 957054-30-7
Catalog number:
Not Intended for Therapeutic Use. For research use only.
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Molecular Weight:
GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K that inhibits p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM.
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B0084-101126 50 mg $199 In stock
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Brife Description:
inhibitor of class I catalytic subunits of PI3K
Related CAS:
957054-33-0 (mesylate)
White to off-white solid powder
4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine; GDC-0941; GDC 0941; GDC0941; RG7321; RG-7321; RG 7321; GNE0941; GNE-0941; GNE 0941; Pictrelisib; Pictilisib
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1.The pan-PI3K inhibitor GDC-0941 activates canonical WNT signaling to confer resistance in TNBC cells: resistance reversal with WNT inhibitor.
Tzeng HE1,2,3,4, Yang L5, Chen K1, Wang Y5, Liu YR6, Pan SL7, Gaur S1, Hu S1, Yen Y1,7. Oncotarget. 2015 May 10;6(13):11061-73.
The pan-PI3K inhibitors are one treatment option for triple-negative breast cancer (TNBC). However, this treatment is ineffective for unknown reasons. Here, we report that aberrant expression of wingless-type MMTV integration site family (WNT) and activated WNT signals, which crosstalk with the PI3K-AKT-mTOR signaling pathway through GSK3β, plays the most critical role in resistance to pan-PI3K inhibitors in TNBC cells. GDC-0941 is a pan-PI3K inhibitor that activates the WNT/beta-catenin pathway in TNBC cells through stimulation of WNT secretion. GDC-0941-triggered WNT/beta-catenin pathway activation was observed in MDA-MB-231 and HCC1937 cells, which are TNBC cell lines showing aberrant WNT/beta-catenin activation, and not in SKBR3 and MCF7 cells. This observation is further investigated in vivo. GDC-0941 exhibited minimal tumor inhibition in MDA-MB-231 cells, but it significantly suppressed tumor growth in HER-positive SK-BR3 cells. In vivo mechanism study revealed the activation of WNT/beta-catenin pathway by GDC-0941.
2.FLT3-ITD confers resistance to the PI3K/Akt pathway inhibitors by protecting the mTOR/4EBP1/Mcl-1 pathway through STAT5 activation in acute myeloid leukemia.
Nogami A1, Oshikawa G1, Okada K1, Fukutake S1, Umezawa Y1, Nagao T1, Kurosu T1, Miura O1. Oncotarget. 2015 Apr 20;6(11):9189-205.
FLT3-ITD and FLT3-TKD are the most frequent tyrosine kinase mutations in acute myeloid leukemia (AML), with the former associated with poor prognosis. Here, we show that the PI3K inhibitor GDC-0941 or the Akt inhibitor MK-2206 induced apoptosis through the mitochondria-mediated intrinsic pathway more efficiently in hematopoietic 32D cells driven by FLT3-TKD (32D/TKD) than FLT3-ITD (32D/ITD), which robustly activated STAT5. The resistance to GDC-0941 and MK-2206 was gained by expression of the constitutively activated STAT5 mutant STAT5A1*6 in 32D/TKD cells, while it was abrogated by the STAT5 inhibitor pimozide in 32D/ITD cells or FLT3-ITD-expressing human leukemic MV4-11 cells. GDC-0941 or MK-2206 induced dephosphorylation of 4EBP1 more conspicuously in 32D/TKD than in 32D/ITD, which was prevented or augmented by STAT5A1*6 or pimozide, respectively, and correlated with downregulation of the eIF4E/eIF4G complex formation and Mcl-1 expression.
3.HBx induced AFP receptor expressed to activate PI3K/AKT signal to promote expression of Src in liver cells and hepatoma cells.
Zhu M1,2, Guo J3, Li W4,5, Xia H6,7, Lu Y8,9, Dong X10,11, Chen Y12,13, Xie X14,15, Fu S16,17, Li M18,19,20. BMC Cancer. 2015 May 6;15:362. doi: 10.1186/s12885-015-1384-9.
BACKGROUND: Hepatitis B virus (HBV)-X protein(HBx) is a transactivator of host several cellular genes including alpha-fetoprotein(AFP) and AFP receptor(AFPR) which contributes to HBV-associated tumor development. The expression of AFP/AFPR are correlated with hepatocellular carcinoma(HCC)-initial cells. But the role of AFP and AFPR in promoting occurrence of HBV-related HCC were still unclear.
4.Immunoaffinity enrichment coupled to quantitative mass spectrometry reveals ubiquitin-mediated signaling events.
Yu K1, Phu L1, Varfolomeev E2, Bustos D1, Vucic D3, Kirkpatrick DS4. J Mol Biol. 2015 Jun 5;427(11):2121-34. doi: 10.1016/j.jmb.2015.03.018. Epub 2015 Apr 8.
Ubiquitination is one of the most prevalent posttranslational modifications in eukaryotic cells, with functional importance in protein degradation, subcellular localization and signal transduction pathways. Immunoaffinity enrichment coupled with quantitative mass spectrometry enables the in-depth characterization of protein ubiquitination events at the site-specific level. We have applied this strategy to investigate cellular response triggered by two distinct type agents: small molecule inhibitors of the tumor-associated kinases MEK and PI3K or the pro-inflammatory cytokine IL-17. Temporal profiling of protein ubiquitination events across a series of time points covering the biological response permits interrogation of signaling through thousands of quantified proteins, of which only a subset display significant and physiologically meaningful regulation. Distinctive clusters of residues within proteins can display distinct temporal patterns attributable to diverse molecular functions, although the majority of differential ubiquitination appears as a coordinated response across the modifiable residues present within an individual substrate.
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CAS 957054-30-7 GDC0941

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