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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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A302849-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $69.90 | |
A302849-1g | 1g | In stock | $147.90 | |
A302849-5g | 5g | In stock | $443.90 | |
A302849-25g | 25g | In stock | $1,329.90 |
Synonyms | Mereletinib | AZD-9291 |
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Specifications & Purity | Moligand™, ≥99% |
Storage Temp | Store at 2-8°C,Desiccated |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Epidermal growth factor receptor erbB1 inhibitor |
Product Description | Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. |
ALogP | 3.7 |
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IUPAC Name | N-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide |
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INCHI | InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32) |
InChi Key | DUYJMQONPNNFPI-UHFFFAOYSA-N |
Canonical SMILES | CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC |
Isomeric SMILES | CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC |
Alternate CAS | 1421373-65-0 |
PubChem CID | 71496458 |
MeSH Entry Terms | AZD-9291;AZD-9291 mesylate;AZD9291;AZD9291 mesylate;mereletinib;mereletinib mesilate;mereletinib mesylate;N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide;N-(2-((2-(dimethylamino |
Molecular Weight | 499.62 |
PubChem CID | 71496458 |
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CAS Registry No. | 1421373-65-0 |
RCSB PDB Ligand | YY3 |
PEP | osimertinib |
Reactome Reaction | R-HSA-9665121, R-HSA-9665280 |
Reactome Drug | R-ALL-9649872 |
DrugCentral Ligand | 5062 |
Enter Lot Number to search for COA:
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Lot Number | Certificate Type | Date | Item |
---|---|---|---|
H2402114 | Certificate of Analysis | Jun 21, 2024 | A302849 |
H2402115 | Certificate of Analysis | Jun 21, 2024 | A302849 |
E2416022 | Certificate of Analysis | Nov 24, 2023 | A302849 |
L2311068 | Certificate of Analysis | Nov 24, 2023 | A302849 |
L2311069 | Certificate of Analysis | Nov 24, 2023 | A302849 |
L2311070 | Certificate of Analysis | Nov 24, 2023 | A302849 |
B2316345 | Certificate of Analysis | Jun 21, 2022 | A302849 |
D2318958 | Certificate of Analysis | Jun 21, 2022 | A302849 |
G2229047 | Certificate of Analysis | Jun 21, 2022 | A302849 |
G2229048 | Certificate of Analysis | Jun 21, 2022 | A302849 |
G2229049 | Certificate of Analysis | Jun 21, 2022 | A302849 |
G2229050 | Certificate of Analysis | Jun 21, 2022 | A302849 |
J2307073 | Certificate of Analysis | Jun 21, 2022 | A302849 |
K2308214 | Certificate of Analysis | Jun 21, 2022 | A302849 |
Solubility | ≥24.98 mg/mL in DMSO; insoluble in H2O; ≥8.09 mg/mL in EtOH with ultrasonic |
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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 |
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 $47.90
1. Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv. (2023) Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115816). [PMID:37976988] |
2. Zihan Zhu, Peigang Zhang, Kexin An, Kaihua Zhao, Xianghui Chen, Yuheng Pei, Martin M. F. Choi, Ning Wang, Wei Bian. (2023) pH/hyaluronidase dual responsive nano drug delivery systems for photothermal/chemotherapy combined treatment for non-small cell lung cancer. NEW JOURNAL OF CHEMISTRY, 47 (46): (21175-21182). [PMID:18487259] |
3. Dianbao Zhang, Yukun Yang, Yixin Kang, Dongjie Xie, Xianfen Zhang, Jiqing Hao. (2023) Dysregulated expression of microRNA involved in resistance to osimertinib in EGFR mutant non-small cell lung cancer cells. Journal of Thoracic Disease, 15 (4): ( 1978–1993). [PMID:37197540] |
1. Yu HA, Riely GJ. (2013) Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in lung cancers.. J Natl Compr Canc Netw, 11 (2): (161-9). [PMID:23411383] |
2. Ou SH, Soo RA. (2015) Dacomitinib in lung cancer: a "lost generation" EGFR tyrosine-kinase inhibitor from a bygone era?. Drug Des Devel Ther, 9 (3): (5641-53). [PMID:26508839] |
3. Song HN, Jung KS, Yoo KH, Cho J, Lee JY, Lim SH, Kim HS, Sun JM, Lee SH, Ahn JS et al.. (2016) Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non-Small Cell Lung Cancer.. J Thorac Oncol, 11 (4): (e45-7). [PMID:26749488] |
4. Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ et al.. (2014) AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.. Cancer Discov, 4 (9): (1046-61). [PMID:24893891] |
5. Wang S, Cang S, Liu D. (2016) Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.. J Hematol Oncol, 9 (3): (34). [PMID:27071706] |
6. Bersanelli M, Minari R, Bordi P, Gnetti L, Bozzetti C, Squadrilli A, Lagrasta CA, Bottarelli L, Osipova G, Capelletto E et al.. (2016) L718Q Mutation as New Mechanism of Acquired Resistance to AZD9291 in EGFR-Mutated NSCLC.. J Thorac Oncol, 11 (10): (e121-3). [PMID:27257132] |
7. Yu HA, Tian SK, Drilon AE, Borsu L, Riely GJ, Arcila ME, Ladanyi M. (2015) Acquired Resistance of EGFR-Mutant Lung Cancer to a T790M-Specific EGFR Inhibitor: Emergence of a Third Mutation (C797S) in the EGFR Tyrosine Kinase Domain.. JAMA Oncol, 1 (7): (982-4). [PMID:26181354] |
8. Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv. (2023) Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115816). [PMID:37976988] |
9. Zihan Zhu, Peigang Zhang, Kexin An, Kaihua Zhao, Xianghui Chen, Yuheng Pei, Martin M. F. Choi, Ning Wang, Wei Bian. (2023) pH/hyaluronidase dual responsive nano drug delivery systems for photothermal/chemotherapy combined treatment for non-small cell lung cancer. NEW JOURNAL OF CHEMISTRY, 47 (46): (21175-21182). [PMID:18487259] |
10. Dianbao Zhang, Yukun Yang, Yixin Kang, Dongjie Xie, Xianfen Zhang, Jiqing Hao. (2023) Dysregulated expression of microRNA involved in resistance to osimertinib in EGFR mutant non-small cell lung cancer cells. Journal of Thoracic Disease, 15 (4): ( 1978–1993). [PMID:37197540] |