Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G126357-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $64.90 | |
G126357-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $97.90 | |
G126357-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $441.90 |
Potent PI3K inhibitor
Synonyms | s7808 | TXCWBWKVIZGWEQ-UHFFFAOYSA-N | HMS3244H10 | HMS3265J06 | Pictilisib [USAN:INN] | s1065 | Pictilisib (USAN) | Q27088388 | 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonyl-1-piperazinyl)methyl]-4-thieno[3,2-d]pyrimidinyl]morpholine | DTXSID40241930 | EC-0 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. GDC-0941 against p110a IC50=0.003μM,U87MG IC50=0.95μM, A2780 IC50=0.14 μM, and in vitro metabolic stability in mouse and human is 91.96%. The |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | PI3-kinase class I inhibitor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2. |
ALogP | 1.6 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[2-(1H-indazol-4-yl)-6-[(4-methylsulfonylpiperazin-1-yl)methyl]thieno[3,2-d]pyrimidin-4-yl]morpholine |
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INCHI | 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) |
InChi Key | LHNIIDJUOCFXAP-UHFFFAOYSA-N |
Canonical SMILES | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 |
Isomeric SMILES | CS(=O)(=O)N1CCN(CC1)CC2=CC3=C(S2)C(=NC(=N3)C4=C5C=NNC5=CC=C4)N6CCOCC6 |
PubChem CID | 17755052 |
Molecular Weight | 513.64 |
CAS Registry No. | 957054-30-7 |
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DiscoveRx TREEspot | GDC-0941| |
ChEBI | CHEBI:65326 |
ChEMBL Ligand | CHEMBL521851 |
PubChem CID | 17755052 |
RCSB PDB Ligand | GD9 |
Reactome Reaction | R-HSA-2400009 |
Reactome Drug | R-ALL-2399804 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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E1704055 | Certificate of Analysis | Dec 08, 2022 | G126357 |
Solubility | DMSO ≥100mg/mL Water ≥103mg/mL Ethanol <1.2mg/mL |
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Refractive Index | 1.75 |
1. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA et al.. (2008) 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, 51 (18): (5522-32). [PMID:18754654] [10.1021/op500134e] |
2. Raynaud FI, Eccles SA, Patel S, Alix S, Box G, Chuckowree I, Folkes A, Gowan S, De Haven Brandon A, Di Stefano F et al.. (2009) Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941.. Mol Cancer Ther, 8 (7): (1725-38). [PMID:19584227] [10.1021/op500134e] |
3. Willemsen-Seegers N, Uitdehaag JCM, Prinsen MBW, de Vetter JRF, de Man J, Sawa M, Kawase Y, Buijsman RC, Zaman GJR. (2017) Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.. J Mol Biol, 429 (4): (574-586). [PMID:28043854] [10.1021/op500134e] |