957054-30-7 | Gdc-0941

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$28.00	$19.00
5mg	95%	in stock	$57.00	$40.00
10mg	95%	in stock	$99.00	$69.00
50mg	95%	in stock	$128.00	$89.00
250mg	95%	in stock	$573.00	$402.00
1g	95%	in stock	$977.00	$684.00

Description

• Catalog Number: AI03469
• Chemical Name: Gdc-0941
• CAS Number: 957054-30-7
• Molecular Formula: C23H27N7O3S2
• Molecular Weight: 513.63558
• MDL Number: MFCD11616196
• SMILES: CS(=O)(=O)N1CCN(CC1)Cc1cc2c(s1)c(nc(n2)c1cccc2c1cn[nH]2)N1CCOCC1

Computed Properties

• Complexity: 832
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 35
• Hydrogen Bond Acceptor Count: 10
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 5
• XLogP3: 1.6

Literature

• Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.

  Journal of molecular biology 20170217

• Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs.

  Toxicological sciences : an official journal of the Society of Toxicology 20150601

• The PI3K inhibitor GDC-0941 combines with existing clinical regimens for superior activity in multiple myeloma.

  Oncogene 20140116

• A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

  Toxicological sciences : an official journal of the Society of Toxicology 20131101

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

  Bioorganic & medicinal chemistry letters 20130801

• PI3K pathway dependencies in endometrioid endometrial cancer cell lines.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20130701

• Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

  Journal of medicinal chemistry 20130613

• Single cell network profiling assay in bladder cancer.

  Cytometry. Part A : the journal of the International Society for Analytical Cytology 20130401

• GDC-0941 enhances the lysosomal compartment via TFEB and primes glioblastoma cells to lysosomal membrane permeabilization and cell death.

  Cancer letters 20130201

• Mechanisms of apoptosis induction by simultaneous inhibition of PI3K and FLT3-ITD in AML cells in the hypoxic bone marrow microenvironment.

  Cancer letters 20130201

• A potent combination of the novel PI3K Inhibitor, GDC-0941, with imatinib in gastrointestinal stromal tumor xenografts: long-lasting responses after treatment withdrawal.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20130201

• Conditional activation of Pik3ca(H1047R) in a knock-in mouse model promotes mammary tumorigenesis and emergence of mutations.

  Oncogene 20130117

• Simultaneous inhibition of pan-phosphatidylinositol-3-kinases and MEK as a potential therapeutic strategy in peripheral T-cell lymphomas.

  Haematologica 20130101

• Phosphoinositide 3-kinase (PI3K) pathway alterations are associated with histologic subtypes and are predictive of sensitivity to PI3K inhibitors in lung cancer preclinical models.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20121215

• Diacylglycerol kinase δ1 transiently translocates to the plasma membrane in response to high glucose.

  Biochimica et biophysica acta 20121201

• PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases.

  Journal of medicinal chemistry 20121025

• Regulation of CD38 expression in human airway smooth muscle cells: role of class I phosphatidylinositol 3 kinases.

  American journal of respiratory cell and molecular biology 20121001

• Phosphatidylinositol 3-kinase/Akt signaling pathway activates the WNK-OSR1/SPAK-NCC phosphorylation cascade in hyperinsulinemic db/db mice.

  Hypertension (Dallas, Tex. : 1979) 20121001

• Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

  Journal of medicinal chemistry 20120913

• Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.

  Molecular cancer therapeutics 20120801

• Harnessing the PI3K/Akt/mTOR pathway in T-cell acute lymphoblastic leukemia: eliminating activity by targeting at different levels.

  Oncotarget 20120801

• GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120715

• Genetic disruption of the PI3K regulatory subunits, p85α, p55α, and p50α, normalizes mutant PTPN11-induced hypersensitivity to GM-CSF.

  Haematologica 20120701

• Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

  Journal of medicinal chemistry 20120628

• Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.

  Journal of medicinal chemistry 20120614

• Gab2 regulates the migratory behaviors and E-cadherin expression via activation of the PI3K pathway in ovarian cancer cells.

  Oncogene 20120517

• Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent.

  Cancer discovery 20120501

• A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.

  Nature chemical biology 20120429

• The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition.

  British journal of cancer 20120410

• Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.

  Bioorganic & medicinal chemistry letters 20120301

• The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.

  Molecular medicine reports 20120201

• Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.

  Anticancer research 20120201

• Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.

  Cancer research 20120101

• Active PI3K pathway causes an invasive phenotype which can be reversed or promoted by blocking the pathway at divergent nodes.

  PloS one 20120101

• The antitumor effect of GDC-0941 alone and in combination with rapamycin in breast cancer cells.

  Chemotherapy 20120101

• Modulators of sensitivity and resistance to inhibition of PI3K identified in a pharmacogenomic screen of the NCI-60 human tumor cell line collection.

  PloS one 20120101

• PI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cells.

  PloS one 20120101

• Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human.

  Xenobiotica; the fate of foreign compounds in biological systems 20111201

• GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.

  The Journal of clinical endocrinology and metabolism 20111201

• Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

  Journal of medicinal chemistry 20111124

• Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

  Journal of medicinal chemistry 20111110

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

• Structural basis for activation and inhibition of class I phosphoinositide 3-kinases.

  Science signaling 20111018

• GDC-0941 sensitizes breast cancer to ABT-737 in vitro and in vivo through promoting the degradation of Mcl-1.

  Cancer letters 20111001

• Essential role of Stat3 in PI3K-induced oncogenic transformation.

  Proceedings of the National Academy of Sciences of the United States of America 20110809

• Preventive and therapeutic effects of phosphoinositide 3-kinase inhibitors on acute lung injury.

  Chest 20110801

• Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.

  Current medicinal chemistry 20110601

• Effect of PI3K- and mTOR-specific inhibitors on spontaneous B-cell follicular lymphomas in PTEN/LKB1-deficient mice.

  British journal of cancer 20110329

• Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR inhibitors: rationale and importance to inhibiting these pathways in human health.

  Oncotarget 20110301

• Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition.

  Cancer letters 20110128

• Liposarcoma: molecular genetics and therapeutics.

  Sarcoma 20110101

• Mutations in the phosphatidylinositol 3-kinase pathway: role in tumor progression and therapeutic implications in breast cancer.

  Breast cancer research : BCR 20110101

• Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

  Chemistry & biology 20101124

• Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption.

  British journal of pharmacology 20101001

• Targeting a common collaborator in cancer development.

  Science translational medicine 20100908

• Nuclear phospho-Akt increase predicts synergy of PI3K inhibition and doxorubicin in breast and ovarian cancer.

  Science translational medicine 20100908

• Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

  Drug metabolism and disposition: the biological fate of chemicals 20100901

• Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

  Drug metabolism and disposition: the biological fate of chemicals 20100901

• Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20100715

• PIKing the right patient.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20100715

• Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

  Bioorganic & medicinal chemistry letters 20100415

• Inhibition profiles of phosphatidylinositol 3-kinase inhibitors against PI3K superfamily and human cancer cell line panel JFCR39.

  European journal of cancer (Oxford, England : 1990) 20100401

• Drugging the PI3 kinome: from chemical tools to drugs in the clinic.

  Cancer research 20100315

• Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

  Journal of medicinal chemistry 20100211

• The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.

  Nature chemical biology 20100201

• Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors.

  Cancer research 20100201

• Physical association of PDK1 with AKT1 is sufficient for pathway activation independent of membrane localization and phosphatidylinositol 3 kinase.

  PloS one 20100101

• Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.

  Molecular cancer therapeutics 20090701

• Suppression of HER2/HER3-mediated growth of breast cancer cells with combinations of GDC-0941 PI3K inhibitor, trastuzumab, and pertuzumab.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20090615

• Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941.

  Cancer cell 20090505

• High-throughput screening compatible cell-based assay for interrogating activated notch signaling.

  Assay and drug development technologies 20090201

• 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 .

  Journal of medicinal chemistry 20080925