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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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A413895-25mg | 25mg | In stock | $61.90 | |
A413895-100mg | 100mg | In stock | $205.90 | |
A413895-500mg | 500mg | In stock | $927.90 | |
A413895-1g | 1g | In stock | $1,668.90 | |
A413895-5g | 5g | In stock | $7,508.90 |
EGFR/ErbB1 Selective Inhibitors | Activators
Synonyms | (R)-4-(3-chloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate | EX-A720 | zorifertinib | (9S,10R)-3,4,5,14,15,16-hexamethoxy-9,10-dimethyltricyclo[10.4.0.0^{2,7}]hexadeca-1(16),2,4,6,12,14-hexaene | 4-((3-Chloro-2-fluo |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Epidermal growth factor receptor erbB1 inhibitor |
Product Description | Information AZD3759 is a potent, oral active, CNS-penetrantEGFRinhibitor withIC50of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. Phase 1. Targets EGFR (L858R) (Cell-free assay); EGFR (exon 19Del) (Cell-free assay); EGFR (WT) (Cell-free assay) 0.2 nM; 0.2 nM; 0.3 nM In vitro In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively, showing mo activity on cell proliferation of H838 cells. In vivo AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy. Cell Research(from reference) Cell lines:PC-9 (exon 19Del), H3255 (L858R) and H838 (wt) cells Concentrations:~30 mM Incubation Time:72 h |
ALogP | 4.635 |
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HBD Count | 1 |
Rotatable Bond | 5 |
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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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Pubchem Sid | 488202379 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488202379 |
IUPAC Name | [4-(3-chloro-2-fluoroanilino)-7-methoxyquinazolin-6-yl] (2R)-2,4-dimethylpiperazine-1-carboxylate |
INCHI | InChI=1S/C22H23ClFN5O3/c1-13-11-28(2)7-8-29(13)22(30)32-19-9-14-17(10-18(19)31-3)25-12-26-21(14)27-16-6-4-5-15(23)20(16)24/h4-6,9-10,12-13H,7-8,11H2,1-3H3,(H,25,26,27)/t13-/m1/s1 |
InChi Key | MXDSJQHFFDGFDK-CYBMUJFWSA-N |
Canonical SMILES | CC1CN(CCN1C(=O)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC)C |
Isomeric SMILES | C[C@@H]1CN(CCN1C(=O)OC2=C(C=C3C(=C2)C(=NC=N3)NC4=C(C(=CC=C4)Cl)F)OC)C |
PubChem CID | 78209992 |
Molecular Weight | 459.9 |
PubChem CID | 78209992 |
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CAS Registry No. | 1626387-80-1 |
ChEMBL Ligand | CHEMBL3623290 |
BindingDB Ligand | 50123453 |
PubChem SID | 488202379 |
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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F2224252 | Certificate of Analysis | Apr 03, 2024 | A413895 |
F2224253 | Certificate of Analysis | Apr 03, 2024 | A413895 |
E23251124 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251125 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251130 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251145 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251156 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251172 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251175 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251179 | Certificate of Analysis | May 06, 2023 | A413895 |
E23251186 | Certificate of Analysis | May 06, 2023 | A413895 |
F2224254 | Certificate of Analysis | May 31, 2022 | A413895 |
F2224255 | Certificate of Analysis | May 31, 2022 | A413895 |
Solubility | Solubility (25°C) In vitro DMSO: 92 mg/mL (200.04 mM); Ethanol: 44 mg/mL warmed with 50ºC Water: bath (95.67 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 91 |
DMSO(mM) Max Solubility | 197.869102 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
Starting at $69.90
1. Zeng Q, Wang J, Cheng Z, Chen K, Johnström P, Varnäs K, Li DY, Yang ZF, Zhang X. (2015) Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.. J Med Chem, 58 (20): (8200-15). [PMID:26313252] [10.1021/op500134e] |