GDC0941 - CAS 957054-30-7
Catalog number:
B0084-101126
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H27N7O3S2
Molecular Weight:
513.635
COA:
Inquire
Targets:
PI3K
Description:
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.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-101126 50 mg $199 In stock
Bulk Inquiry
Publictions citing BOC Sciences Products
  • >> More
Brife Description:
inhibitor of class I catalytic subunits of PI3K
Related CAS:
957054-33-0 (mesylate)
Appearance:
White to off-white solid powder
Synonyms:
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
MSDS:
Inquire
InChIKey:
LHNIIDJUOCFXAP-UHFFFAOYSA-N
InChI:
1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
Canonical SMILES:
O=S(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)(C)=O
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related PI3K Products


CAS 956958-53-5 XL147

XL147
(CAS: 956958-53-5)

Pilaralisib is a Class 1 phosphatidylinositol 3 kinase (PI3K) family inhibitor. It is an orally bioavailable small molecule, targeting the class I PI3K family o...

CAS 474012-90-3 CAL-130 Racemate

CAL-130 Racemate
(CAS: 474012-90-3)

CAL-130 racemate is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphobla...

CAS 1252594-99-2 ETP-46321

ETP-46321
(CAS: 1252594-99-2)

ETP-46321 is a potent and orally bioavailable PI3K α, δ inhibitor with potent biochemical and cellular activity and good pharmacokinetic properties (PK) after o...

CAS 957209-68-6 NVP-QAV-572

NVP-QAV-572
(CAS: 957209-68-6)

NVP-QAV-572 is a potent PI3K kianse inhibitor.

CAS 944396-07-0 BKM120

BKM120
(CAS: 944396-07-0)

BKM120, also called as buparlisib or NVP-BKM120, activity in a range of preclinical cancermodels, specifically inhbits class I PI3K isoforms, which blocks p110α...

CAS 1236188-16-1 740 Y-P

740 Y-P
(CAS: 1236188-16-1)

740 Y-P is a cell-permeable phosphopeptide activator of PI3K. It binds to the p85 N- and C-terminal SH2 domains of PI3K but not to GST or the N-terminal domain ...

CAS 677338-12-4 PIK-90

PIK-90
(CAS: 677338-12-4)

PIK-90 is a potent PI3K inhibitor.

CAS 1159824-67-5 CZC24832

CZC24832
(CAS: 1159824-67-5)

CZC24832 is the first selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with efficacy in in vitro and in vivo models of inflammation. Extensive target-...

CAS 1383716-33-3 VPS34-IN1

VPS34-IN1
(CAS: 1383716-33-3)

VPS34-IN1 is a potent and selective Vps34 inhibitor with potential anticancer activity. VPS34-IN1 inhibits Vps34 with 25 nM IC50 in vitro.

CAS 1383716-46-8 VPS34 inhibitor 1

VPS34 inhibitor 1
(CAS: 1383716-46-8)

VPS34 inhibitor 1 is a potent and selective inhibitor of VPS34 (IC50= 15 nM). Vps34 is a phosphoinositide 3-kinase (PI3K) class III isoform that has attracted m...

CAS 1254036-66-2 GSK2292767

GSK2292767
(CAS: 1254036-66-2)

GSK2292767 is a Phosphatidylinositol 3 kinase delta inhibitor applicated for the treatment of respiratory diseases including asthma and COPD in clinical trials....

CAS 5142-23-4 NSC 66389,3-MA

NSC 66389,3-MA
(CAS: 5142-23-4)

PQR309
(CAS: 1225037-39-7)

PQR309, a pan inhibitor of phosphoinositide-3-kinases, is still under Phase II clinical trial against Glioblastoma and Lymphoma.

CAS 1702816-75-8 PI3Kδ-IN-2

PI3Kδ-IN-2
(CAS: 1702816-75-8)

PI3Kδ-IN-2 is a potent and selective inhibitor ofPI3Kδ (IC50= 6.4 M).

CAS 1431697-78-7 CAL-130 Hydrochloride

CAL-130 Hydrochloride
(CAS: 1431697-78-7)

In the absence of PTEN phosphatase tumor suppressor function, PI3Kγ or PI3Kδ alone can support leukemogenesis, whereas inactivation of both isoforms suppressed ...

CAS 1246560-33-7 VS-5584

VS-5584
(CAS: 1246560-33-7)

LY-3023414
(CAS: 1386874-06-1)

LY3023414, a quinoline derivative, has been found to be a PI3Kα and mTOR inhibitor that could influence cell proliferation and cycle of tumor cells. It was just...

CAS 1404231-34-0 ON 146040

ON 146040
(CAS: 1404231-34-0)

ON 146040 was highly potent in killing hematologic tumor cells with IC50 values in the 150 to 1,000 nM range. In biochemical testing, ON 146040 inhibited PI3K α...

CAS 1383716-40-2 Vps34-PIK-III

Vps34-PIK-III
(CAS: 1383716-40-2)

Vps34-PIK-III is a potent and selective inhibitor of the type 3 phosphatidylinositol 3-kinase (PI3K) vacuolar protein sorting 34 (Vps34) (IC50= 18 nM). Vps34-PI...

PQR530
(CAS: 1927857-61-1)

PQR530 is a potent dual pan PI3K/mTOR inhibitor undergoing phase II clinical trials in 2016. Aberrant activation of the PI3K/mTOR signaling pathway promotes the...

Chemical Structure

CAS 957054-30-7 GDC0941

Quick Inquiry

Verification code

Featured Items