GDC-0941 (Pictilisib)
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201395

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

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.


Price and Availability

Size
Price

5mg
USD 90
50mg
USD 250
500mg
USD 1650
5g
USD 4950
Size
Price

10mg
USD 120
100mg
USD 450
1g
USD 1950
10g
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Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 2950
20g
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GDC-0941 (Pictilisib), purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 201395
Name: GDC-0941 (Pictilisib)
CAS#: 957054-30-7 (free base); 957054-33-0 (mesylate).
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


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 Key: LHNIIDJUOCFXAP-UHFFFAOYSA-N

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)

SMILES Code: O=S(N1CCN(CC2=CC3=NC(C4=CC=CC5=C4C=NN5)=NC(N6CCOCC6)=C3S2)CC1)(C)=O


Technical Data

Appearance:
White to off-white solid powder

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

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Solubility:
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).

Harmonized System Code:
293490


References

1: Ehrhardt M, Craveiro RB, Holst MI, Pietsch T, Dilloo D. The PI3K inhibitor GDC-0941 displays promising in vitro and in vivo efficacy for targeted medulloblastoma therapy. Oncotarget. 2015 Jan 20;6(2):802-13. PubMed PMID: 25596739.

2: Sarker D, Ang JE, Baird R, Kristeleit R, Shah K, Moreno V, Clarke PA, Raynaud FI, Levy G, Ware JA, Mazina K, Lin R, Wu J, Fredrickson J, Spoerke JM, Lackner MR, Yan Y, Friedman LS, Kaye SB, Derynck MK, Workman P, de Bono JS. First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors. Clin Cancer Res. 2015 Jan 1;21(1):77-86. doi: 10.1158/1078-0432.CCR-14-0947. Epub 2014 Nov 4. PubMed PMID: 25370471; PubMed Central PMCID: PMC4287394.

3: Salphati L, Shahidi-Latham S, Quiason C, Barck K, Nishimura M, Alicke B, Pang J, Carano RA, Olivero AG, Phillips HS. Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging. Drug Metab Dispos. 2014 Jul;42(7):1110-6. doi: 10.1124/dmd.114.057513. Epub 2014 Apr 22. PubMed PMID: 24754926.

4: Zheng J, Wang H, Yao J, Zou X. More antitumor efficacy of the PI3K inhibitor GDC-0941 in breast cancer with PIK3CA mutation or HER2 amplification status in vitro. Pharmazie. 2014 Jan;69(1):38-42. PubMed PMID: 24601221.

5: Ware JA, Dalziel G, Jin JY, Pellett JD, Smelick GS, West DA, Salphati L, Ding X, Sutton R, Fridyland J, Dresser MJ, Morrisson G, Holden SN. Impact of food and the proton pump inhibitor rabeprazole on the pharmacokinetics of GDC-0941 in healthy volunteers: bench to bedside investigation of pH-dependent solubility. Mol Pharm. 2013 Nov 4;10(11):4074-81. doi: 10.1021/mp4005595. Epub 2013 Oct 24. PubMed PMID: 24099279.

6: Pang J, Dalziel G, Dean B, Ware JA, Salphati L. Pharmacokinetics and absorption of the anticancer agents dasatinib and GDC-0941 under various gastric conditions in dogs--reversing the effect of elevated gastric pH with betaine HCl. Mol Pharm. 2013 Nov 4;10(11):4024-31. doi: 10.1021/mp400356m. Epub 2013 Sep 11. PubMed PMID: 23980865.

7: Jin L, Tabe Y, Kojima K, Shikami M, Benito J, Ruvolo V, Wang RY, McQueen T, Ciurea SO, Miida T, Andreeff M, Konopleva M. PI3K inhibitor GDC-0941 enhances apoptotic effects of BH-3 mimetic ABT-737 in AML cells in the hypoxic bone marrow microenvironment. J Mol Med (Berl). 2013 Dec;91(12):1383-97. doi: 10.1007/s00109-013-1076-3. Epub 2013 Aug 18. PubMed PMID: 23955073; PubMed Central PMCID: PMC3834093.

8: Cawthorne C, Burrows N, Gieling RG, Morrow CJ, Forster D, Gregory J, Radigois M, Smigova A, Babur M, Simpson K, Hodgkinson C, Brown G, McMahon A, Dive C, Hiscock D, Wilson I, Williams KJ. [18F]-FLT positron emission tomography can be used to image the response of sensitive tumors to PI3-kinase inhibition with the novel agent GDC-0941. Mol Cancer Ther. 2013 May;12(5):819-28. doi: 10.1158/1535-7163.MCT-12-0905. Epub 2013 Feb 20. PubMed PMID: 23427298; PubMed Central PMCID: PMC3670082.

9: Munugalavadla V, Mariathasan S, Slaga D, Du C, Berry L, Del Rosario G, Yan Y, Boe M, Sun L, Friedman LS, Chesi M, Leif Bergsagel P, Ebens A. The PI3K inhibitor GDC-0941 combines with existing clinical regimens for superior activity in multiple myeloma. Oncogene. 2014 Jan 16;33(3):316-25. doi: 10.1038/onc.2012.594. Epub 2013 Jan 14. PubMed PMID: 23318440.

10: Floris G, Wozniak A, Sciot R, Li H, Friedman L, Van Looy T, Wellens J, Vermaelen P, Deroose CM, Fletcher JA, Debiec-Rychter M, Schöffski P. A potent combination of the novel PI3K Inhibitor, GDC-0941, with imatinib in gastrointestinal stromal tumor xenografts: long-lasting responses after treatment withdrawal. Clin Cancer Res. 2013 Feb 1;19(3):620-30. doi: 10.1158/1078-0432.CCR-12-2853. Epub 2012 Dec 11. PubMed PMID: 23231951.