GDC-0941

Modify Date: 2024-01-02 12:12:06

GDC-0941 structure	Common Name	GDC-0941
	CAS Number	957054-30-7	Molecular Weight	513.636
	Density	1.5±0.1 g/cm3	Boiling Point	687.7±65.0 °C at 760 mmHg
	Molecular Formula	C₂₃H₂₇N₇O₃S₂	Melting Point	N/A
	MSDS	N/A	Flash Point	369.7±34.3 °C

Use of GDC-0941

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).

Name	pictrelisib
Synonym	More Synonyms

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).
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> PI3K/Akt/mTOR >> PI3K Research Areas >> Cancer
Target	p110α:3 nM (IC50) p110α-H1047R:3 nM (IC50) p110α-E545K:3 nM (IC50) p110δ:3 nM (IC50) p110β:33 nM (IC50) p110γ:75 nM (IC50) mTOR:0.58 μM (Ki) DNA-PK:1.23 μM (IC50) Autophagy
In Vitro	GDC-0941 and docetaxel reduce tumor cell viability by 80% or greater in the breast cancer cell lines than single-agent treatment. GDC-0941 inhibits Akt phosphorylation and downstream targets of Akt signaling such as pPRAS40 and pS6 in Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null) tumor models. GDC-0941 decreases the time of docetaxel-induced mitotic arrest prior to apoptosis[1]. GDC-0941 shows a high efficacy of antitumor activity in two gefitinib-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. GDC-0941 is highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest and cell apoptosis. H460 cells with activating mutations of PIK3CA are relatively more sensitive to GDC-0941 than A549 cells with wild-type PIK3CA[3]. GDC-0941 reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. GDC-0941 significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells[4].
In Vivo	GDC-0941 (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. GDC-0941 and docetaxel result in tumor regressions during the treatment period leading to enhanced antitumor responses[1]. Tumours in the GDC-0941-treated mice show a marked non-linear shrinkage, and when the GDC-0941 treatment ceased, the tumours in the test cohort mice grow again[2]. GDC-0941 (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice[4].
Cell Assay	Cells are treated at EC50 concentrations of GDC-0941, docetaxel, or both for 4 or 24 hours and lysed in 1×Cell Extraction Buffer supplemented with protease inhibitors and Phosphatase Inhibitor Cocktails 1 and 2. Protein concentrations are determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal amounts of protein are separated by electrophoresis through NuPAGE Bis-Tris 10% gradient gels, transferred onto polyvinylidene difluoride membranes using the Criterion system, and probed with monospecific primary antibodies. Specific antigen-antibody interactions are detected with IRDye 680 or IRDye 800 infrared secondary antibodies using a LI-COR imaging system.
Animal Admin	Female nu/nu mice are inoculated subcutaneously with MCF7-neo/HER2 or MX-1 breast cancer cells. When tumors reach a mean volume of 200 to 250 mm3, animals are size-matched and distributed into groups consisting of 10 animals per group. Docetaxel formulated in 3% EtOH, 97% saline is administered intravenously once weekly. GDC-0941, formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) is dosed orally and daily. MAXF1162 is an HER2+/ER+/PR+ patient-derived breast cancer tumor xenograft model established by directly implanting tumors subcutaneously from patient to NMRI nu/nu mice. Tumor volume is calculated. Tumor sizes are recorded twice weekly over the course of a study.
References	[1]. Wallin JJ, et al. 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.Clin Cancer Res. 2012 Jul 15;18(14):3901-11. Epub 2012 May 14. [2]. Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32(2):415-20. [3]. Zou ZQ, et al. The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5(2):503-8. [4]. Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96(12):E1934-43. Epub 2011 Oct [5]. Folkes AJ, et al. 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. 2008 Sep 25;51(18):5522-32. [6]. Ni J, et al. Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov. 2012 May;2(5):425-33. [7]. Cheng H, et al. A genetic mouse model of invasive endometrial cancer driven by concurrent loss of Pten and Lkb1 Is highly responsive to mTOR inhibition. Cancer Res. 2014 Jan 1;74(1):15-23.

Density	1.5±0.1 g/cm3
Boiling Point	687.7±65.0 °C at 760 mmHg
Molecular Formula	C₂₃H₂₇N₇O₃S₂
Molecular Weight	513.636
Flash Point	369.7±34.3 °C
Exact Mass	513.161682
PSA	144.17000
LogP	2.04
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.753

HS Code	29350090

Precursor 10
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DownStream 0

4-(2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine

pictrelisib

Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-

GDC0941

GDC-941

GDC 0941

2-(1H-Indazol-4-yl)-6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin

2-(1H-Indazol-4-yl)-6-{[4-(methylsulfonyl)-1-piperazinyl]methyl}-4-(4-morpholinyl)thieno[3,2-d]pyrimidine

Pictilisib

2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine

GDC-0941

GDC-0941 bismesylate

DC Chemicals Limited
China
Product Name: GDC0941(Pictilisib)
Price: $400.0/100mg $800.0/250mg $1450.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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Price: ￥390/10mg

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