GDC-0941 (Pictilisib)

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201395

CAS#: 957054-30-7 (free base)

Description: Pictilisib, also known as Pictrelisib, GDC-0941, RG7321 and GNE0941 , is an orally bioavailable, and is a potent small-molecule thieno[3,2-d]pyrimidine inhibitor of the class I phosphatidylinositol 3 kinase (PI3K) isoforms p100alpha and p100delta with potential antineoplastic activity. PI3K inhibitor GDC-0941 selectively binds to PI3K isoforms in an ATP-competitive manner, inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway; inhibition of tumor cell growth, motility and survival in susceptible tumor cell populations may result.

Chemical Structure

GDC-0941 (Pictilisib)
CAS# 957054-30-7 (free base)

Theoretical Analysis

MedKoo Cat#: 201395
Name: GDC-0941 (Pictilisib)
CAS#: 957054-30-7 (free base)
Chemical Formula: C23H27N7O3S2
Exact Mass: 513.16168
Molecular Weight: 513.63
Elemental Analysis: C, 53.78; H, 5.30; N, 19.09; O, 9.34; S, 12.49

Size Price Shipping out time Quantity
100mg USD 150 Same day
200mg USD 250 Same day
500mg USD 450 Same day
1g USD 750 Same day
2g USD 1250 Same day
5g USD 2650 Same day
10g USD 4650 2 weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

GDC-0941 (Pictilisib), purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 957054-30-7 (free base)   957054-33-0 (mesylate)  

Synonym: GDC-0941; GDC 0941; GDC0941; RG7321; RG-7321; RG 7321; GNE0941; GNE-0941; GNE 0941; Pictrelisib; Pictilisib

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


InChi Code: 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)


White to off-white solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Preparing Stock Solutions

The following data is based on the product molecular weight 513.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: De Wolf E, De Wolf C, Richardson A. ABT-737 and pictilisib synergistically enhance pitavastatin-induced apoptosis in ovarian cancer cells. Oncol Lett. 2018 Feb;15(2):1979-1984. doi: 10.3892/ol.2017.7516. Epub 2017 Dec 5. PubMed PMID: 29434898; PubMed Central PMCID: PMC5778268.

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3: Langhans J, Schneele L, Trenkler N, von Bandemer H, Nonnenmacher L, Karpel-Massler G, Siegelin MD, Zhou S, Halatsch ME, Debatin KM, Westhoff MA. The effects of PI3K-mediated signalling on glioblastoma cell behaviour. Oncogenesis. 2017 Nov 29;6(11):398. doi: 10.1038/s41389-017-0004-8. PubMed PMID: 29184057.

4: Yang W, Hosford SR, Traphagen NA, Shee K, Demidenko E, Liu S, Miller TW. Autophagy promotes escape from phosphatidylinositol 3-kinase inhibition in estrogen receptor-positive breast cancer. FASEB J. 2018 Jan 3:fj201700477R. doi: 10.1096/fj.201700477R. [Epub ahead of print] PubMed PMID: 29127189.

5: Soria JC, Adjei AA, Bahleda R, Besse B, Ferte C, Planchard D, Zhou J, Ware J, Morrissey K, Shankar G, Lin W, Schutzman JL, Dy GK, Groen HJM. A phase IB dose-escalation study of the safety and pharmacokinetics of pictilisib in combination with either paclitaxel and carboplatin (with or without bevacizumab) or pemetrexed and cisplatin (with or without bevacizumab) in patients with advanced non-small cell lung cancer. Eur J Cancer. 2017 Nov;86:186-196. doi: 10.1016/j.ejca.2017.08.027. Epub 2017 Oct 6. PubMed PMID: 28992562.

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7: Chen J, Guo J, Cui X, Dai Y, Tang Z, Qu J, Raj JU, Hu Q, Gou D. The Long Noncoding RNA LnRPT Is Regulated by PDGF-BB and Modulates the Proliferation of Pulmonary Artery Smooth Muscle Cells. Am J Respir Cell Mol Biol. 2018 Feb;58(2):181-193. doi: 10.1165/rcmb.2017-0111OC. PubMed PMID: 28915060.

8: Zeng SX, Zhu Y, Ma AH, Yu W, Zhang H, Lin TY, Shi W, Tepper CG, Henderson PT, Airhart S, Guo JM, Xu CL, deVere White RW, Pan CX. The Phosphatidylinositol 3-Kinase Pathway as a Potential Therapeutic Target in Bladder Cancer. Clin Cancer Res. 2017 Nov 1;23(21):6580-6591. doi: 10.1158/1078-0432.CCR-17-0033. Epub 2017 Aug 14. PubMed PMID: 28808038; PubMed Central PMCID: PMC5668181.

9: Leong S, Moss RA, Bowles DW, Ware JA, Zhou J, Spoerke JM, Lackner MR, Shankar G, Schutzman JL, van der Noll R, Voest EE, Schellens JHM. A Phase I Dose-Escalation Study of the Safety and Pharmacokinetics of Pictilisib in Combination with Erlotinib in Patients with Advanced Solid Tumors. Oncologist. 2017 Dec;22(12):1491-1499. doi: 10.1634/theoncologist.2017-0090. Epub 2017 Aug 10. PubMed PMID: 28798270; PubMed Central PMCID: PMC5728021.

10: Lu T, Fraczkiewicz G, Salphati L, Budha N, Dalziel G, Smelick GS, Morrissey KM, Davis JD, Jin JY, Ware JA. Combining "Bottom-up" and "Top-down" Approaches to Assess the Impact of Food and Gastric pH on Pictilisib (GDC-0941) Pharmacokinetics. CPT Pharmacometrics Syst Pharmacol. 2017 Nov;6(11):747-755. doi: 10.1002/psp4.12228. Epub 2017 Oct 17. PubMed PMID: 28748626; PubMed Central PMCID: PMC5702897.

11: Nathan MR, Schmid P. A Review of Fulvestrant in Breast Cancer. Oncol Ther. 2017;5(1):17-29. doi: 10.1007/s40487-017-0046-2. Epub 2017 May 8. Review. PubMed PMID: 28680952; PubMed Central PMCID: PMC5488136.

12: Dogan T, Gnad F, Chan J, Phu L, Young A, Chen MJ, Doll S, Stokes MP, Belvin M, Friedman LS, Kirkpatrick DS, Hoeflich KP, Hatzivassiliou G. Role of the E3 ubiquitin ligase RNF157 as a novel downstream effector linking PI3K and MAPK signaling pathways to the cell cycle. J Biol Chem. 2017 Sep 1;292(35):14311-14324. doi: 10.1074/jbc.M117.792754. Epub 2017 Jun 27. PubMed PMID: 28655764; PubMed Central PMCID: PMC5582827.

13: Zheng X, Goodwin AF, Tian H, Jheon AH, Klein OD. Ras Signaling Regulates Stem Cells and Amelogenesis in the Mouse Incisor. J Dent Res. 2017 Nov;96(12):1438-1444. doi: 10.1177/0022034517717255. Epub 2017 Jun 23. PubMed PMID: 28644741; PubMed Central PMCID: PMC5652855.

14: Rewcastle GW, Kolekar S, Buchanan CM, Gamage SA, Giddens AC, Tsang KY, Kendall JD, Singh R, Lee WJ, Smith GC, Han W, Matthews DJ, Denny WA, Shepherd PR, Jamieson SMF. Biological characterization of SN32976, a selective inhibitor of PI3K and mTOR with preferential activity to PI3Kα, in comparison to established pan PI3K inhibitors. Oncotarget. 2017 Jul 18;8(29):47725-47740. doi: 10.18632/oncotarget.17730. PubMed PMID: 28537878; PubMed Central PMCID: PMC5564600.

15: Zhan M, Deng Y, Zhao L, Yan G, Wang F, Tian Y, Zhang L, Jiang H, Chen Y. Design, Synthesis, and Biological Evaluation of Dimorpholine Substituted Thienopyrimidines as Potential Class I PI3K/mTOR Dual Inhibitors. J Med Chem. 2017 May 11;60(9):4023-4035. doi: 10.1021/acs.jmedchem.7b00357. Epub 2017 Apr 24. PubMed PMID: 28409639.

16: Masson GR, Maslen SL, Williams RL. Analysis of phosphoinositide 3-kinase inhibitors by bottom-up electron-transfer dissociation hydrogen/deuterium exchange mass spectrometry. Biochem J. 2017 May 16;474(11):1867-1877. doi: 10.1042/BCJ20170127. PubMed PMID: 28381646; PubMed Central PMCID: PMC5544108.

17: Wang Y, Li J, Chen JJ, Gao X, Huang Z, Shen Q. Multifunctional Nanoparticles Loading with Docetaxel and GDC0941 for Reversing Multidrug Resistance Mediated by PI3K/Akt Signal Pathway. Mol Pharm. 2017 Apr 3;14(4):1120-1132. doi: 10.1021/acs.molpharmaceut.6b01045. Epub 2017 Mar 22. PubMed PMID: 28291364.

18: Shi F, Guo H, Zhang R, Liu H, Wu L, Wu Q, Liu J, Liu T, Zhang Q. The PI3K inhibitor GDC-0941 enhances radiosensitization and reduces chemoresistance to temozolomide in GBM cell lines. Neuroscience. 2017 Mar 27;346:298-308. doi: 10.1016/j.neuroscience.2017.01.032. Epub 2017 Jan 29. PubMed PMID: 28147244.

19: Packer LM, Geng X, Bonazzi VF, Ju RJ, Mahon CE, Cummings MC, Stephenson SA, Pollock PM. PI3K Inhibitors Synergize with FGFR Inhibitors to Enhance Antitumor Responses in FGFR2(mutant) Endometrial Cancers. Mol Cancer Ther. 2017 Apr;16(4):637-648. doi: 10.1158/1535-7163.MCT-16-0415. Epub 2017 Jan 23. PubMed PMID: 28119489.

20: Soler A, Figueiredo AM, Castel P, Martin L, Monelli E, Angulo-Urarte A, Milà-Guasch M, Viñals F, Baselga J, Casanovas O, Graupera M. Therapeutic Benefit of Selective Inhibition of p110α PI3-Kinase in Pancreatic Neuroendocrine Tumors. Clin Cancer Res. 2016 Dec 1;22(23):5805-5817. Epub 2016 May 25. PubMed PMID: 27225693; PubMed Central PMCID: PMC5338478.