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

Name: Pictilisib dimethanesulfonate
Brand: MedChemExpress
SKU: HY-20180
Rating: 5.0 (58 reviews)

Cat. No.: HY-20180 Purity: 99.72%: FAQs
Data Sheet SDS COA Handling Instructions

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Pictilisib dimethanesulfonate (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.

Pictilisib dimethanesulfonate Chemical Structure

CAS No. : 957054-33-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
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200 mg	USD 252	In-stock	Estimated Time of Arrival: December 31
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Based on 58 publication(s) in Google Scholar

Other Forms of Pictilisib dimethanesulfonate:

Pictilisib In-stock

48 Publications Citing Use of MCE Pictilisib dimethanesulfonate

Proliferation Assay

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Sep;51(3):823-831. [Abstract]; Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2016 Feb 2;7:10438. [Abstract]; Western blot illustrating the effect of PI3K inhibitors on p21 protein levels in MEFs. Cells are treated for 24 hours with the indicated concentrations of the different drugs.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70. [Abstract]; Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC⁺PIK3CA^H1047R tumors treated as indicated.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]; PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]; The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC₅₀ of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Ectopic expression of LKB1 renders PTEN LKB1-deficient endometrial cancer cells susceptible to PI3K inhibition. Western blot analysis of pS6RP (Ser235/236) and p4EBP1(Ser65) in ETN-1 and HEC108 cells with stable expression of vector or flag- tagged LKB1. Cell lysates were harvested 24 hours after GDC-0941 treatment.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23. [Abstract]; Differential responses of Pten Lkb1-deficient endometrial tumors to inhibitors targeting PI3K and/or mTOR. Mice bearing transplanted Pten Lkb1-deficient endometrial tumors are treated with indicated drugs for 3 days and sacrificed three hours after their dose on day 3 of treatment; their tumors are isolated and tumor lysates are immunoblotted with the indicated antibodies.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99. [Abstract]; Sensitivity to GDC-0941 in parental MDA453 and T47D and BYL719-resistant MDA453R and T47DR cells. Protein lysates are isolated after 24 hours of treatment with 1 μM GDC-0941 and probed against the indicated proteins.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cell Metab. 2012 Mar 7;15(3):382-94. [Abstract]; Effect of the indicated PI3K inhibitors on pre-brown adipocytes. Cultures are treated with the inhibitors at the indicated concentrations (μM) for 4 h. Protein levels (top) and mRNA levels (bottom) of the indicated proteins and genes, respectively, are analyzed. Assays are performed in triplicate cultures. Values represent mean ± sd, and statistical significance is determined by the two-tailed Student’s t-test. *p<0.05, **p<0.01.

: Pictilisib dimethanesulfonate purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33. [Abstract]; Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Pictilisib dimethanesulfonate (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^[5]

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

Pictilisib (GDC-0941) and RP-56976 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. Pictilisib (GDC-0941) decreases the time of RP-56976-induced mitotic arrest prior to apoptosis^[1]. Pictilisib (GDC-0941) shows a high efficacy of antitumor activity in two ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. Pictilisib (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 Pictilisib (GDC-0941) than A549 cells with wild-type PIK3CA^[3]. Pictilisib (GDC-0941) reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. Pictilisib (GDC-0941) significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pictilisib (GDC-0941) (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. Pictilisib (GDC-0941) and RP-56976 result in tumor regressions during the treatment period leading to enhanced antitumor responses^[1]. Tumours in the Pictilisib (GDC-0941)-treated mice show a marked non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again^[2]. GDC-0941Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

705.85

Formula

C₂₅H₃₅N₇O₉S₄

CAS No.

957054-33-0

Appearance

Solid

Color

White to light yellow

SMILES

O=S(N1CCN(CC1)CC2=CC3=C(S2)C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)(C)=O.O=S(O)(C)=O.O=S(O)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 7.14 mg/mL (10.12 mM; ultrasonic and warming and heat to 60°C)

DMSO : 7.14 mg/mL (10.12 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.72%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (251 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 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. [Content Brief]

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. 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 [Content Brief]

Cell Assay ^[1]	Cells are treated at EC₅₀ concentrations of Pictilisib (GDC-0941), RP-56976, 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]	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. RP-56976 formulated in 3% EtOH, 97% saline is administered intravenously once weekly. Pictilisib (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	[1]. Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 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. [Content Brief] [2]. 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. [Content Brief] [3]. 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. [Content Brief] [4]. 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. [Content Brief] [5]. 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 [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.4167 mL	7.0837 mL	14.1673 mL	35.4183 mL
	5 mM	0.2833 mL	1.4167 mL	2.8335 mL	7.0837 mL
	10 mM	0.1417 mL	0.7084 mL	1.4167 mL	3.5418 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Pictilisib dimethanesulfonate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pictilisib957054-33-0GDC-0941GDC-0941 2 MeSO3HGDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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

Customer Review

Other Forms of Pictilisib dimethanesulfonate:

Pictilisib dimethanesulfonate Related Antibodies

48 Publications Citing Use of MCE Pictilisib dimethanesulfonate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Pictilisib dimethanesulfonate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Pictilisib dimethanesulfonate Related Classifications

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