1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    Autophagy

GDC-0941 dimethanesulfonate (Synonyms: Pictilisib dimethanesulfonate; GDC-0941 (2 MeSO3H salt); GDC-0941)

Cat. No.: HY-20180 Purity: 99.12%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
GDC-0941 dimethanesulfonate Chemical Structure

GDC-0941 dimethanesulfonate Chemical Structure

CAS No. : 957054-33-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $75 In-stock
100 mg $120 In-stock
200 mg $210 In-stock
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Other Forms of GDC-0941 dimethanesulfonate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 3 nM (PI3Kα), 3 nM (PI3Kδ)[5]

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.4167 mL 7.0837 mL 14.1673 mL
5 mM 0.2833 mL 1.4167 mL 2.8335 mL
10 mM 0.1417 mL 0.7084 mL 1.4167 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

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[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

GDC-0941 is formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) (Mice)[1].

Mice[1]
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.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

705.85

Formula

C₂₅H₃₅N₇O₉S₄

CAS No.

957054-33-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.12%

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Product Name:
GDC-0941 dimethanesulfonate
Cat. No.:
HY-20180
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