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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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P125961-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $84.90 | |
P125961-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $260.90 | |
P125961-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $469.90 |
Synonyms | GTPL5701 | PI 103 hydrobromide | 3-(4-(4-morpholinyl)pyrido[3?,2?:4,5]furo[3,2-d]pyrimidin-2- yl)phenol | 3-(4-morpholinopyrido[2,3]furo[2,4-b]pyrimidin-2-yl)phenol | AC-31514 | BDBM25045 | NSC 81361 | 3-(6-morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK, PI 3-kinase (Class IA), and FRAP (mTOR) complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of mechanistic target of rapamycin kinase;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4; |
Note | 卖完停产,不再备货 |
Product Description | PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. |
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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 | 3-(6-morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)phenol |
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INCHI | InChI=1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2 |
InChi Key | TUVCWJQQGGETHL-UHFFFAOYSA-N |
Canonical SMILES | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O |
Isomeric SMILES | C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O |
PubChem CID | 9884685 |
Molecular Weight | 348.36 |
CAS Registry No. | 371935-74-9 |
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PubChem CID | 9884685 |
DiscoveRx TREEspot | PI-103| |
ChEMBL Ligand | CHEMBL573339 |
RCSB PDB Ligand | X6K |
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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I1509076 | Certificate of Analysis | Mar 17, 2023 | P125961 |
Solubility | Soluble in DMSO (10 mg/ml), DMF (10 mg/ml), 1:2 DMSO:PBS(pH 7.2) (0.25 mg/ml), water (<1 mg/ml) at 25 °C, and ethanol (<1 mg/ml) at 25 °C. |
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1. Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B et al.. (2006) A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.. Cell, 125 (4): (733-47). [PMID:16647110] [10.1021/op500134e] |
2. Fan QW, Knight ZA, Goldenberg DD, Yu W, Mostov KE, Stokoe D, Shokat KM, Weiss WA. (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.. Cancer Cell, 9 (5): (341-9). [PMID:16697955] [10.1021/op500134e] |
3. Hayakawa M, Kaizawa H, Moritomo H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI et al.. (2007) Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.. Bioorg Med Chem Lett, 17 (9): (2438-42). [PMID:17339109] [10.1021/op500134e] |
4. 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] |