EGF816 - CAS 1508250-71-2
Catalog number: B0084-474599
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C26H31ClN6O2
Molecular Weight:
495.02
COA:
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Targets:
EGFR
Description:
EGF816, also called as Nazartinib, a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M resistance mutation while sparing wild-type EGFR. in vivo: demonstrated strong tumor regressions in several EGFR activating and resistant tumor m
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474599 10 mg $149 In stock
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Appearance:
Solid powder
Synonyms:
EGF816; EGF-816; EGF 816; NVS-816; NVS 816; NVS816; Nazartinib; N-[7-chloro-1-[(3R)-1-[(E)-4-(dimethylamino)but-2-enoyl]azepan-3-yl]benzimidazol-2-yl]-2-methylpyridine-4-carboxamideEGF816UNII-KE7K32EME8KE7K32EME8EGF-8161508250-71-2GTPL9204SCHEMBL16767232SCHEMBL16767240EGF 816compound 47 [PMID: 27433829]
Solubility:
Soluble in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -45℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Quantity:
Grams-Kilos
Density:
1.28±0.1 g/cm3
InChIKey:
IOMMMLWIABWRKL-WUTDNEBXSA-N
InChI:
1S/C26H31ClN6O2/c1-18-16-19(12-13-28-18)25(35)30-26-29-22-10-6-9-21(27)24(22)33(26)20-8-4-5-15-32(17-20)23(34)11-7-14-31(2)3/h6-7,9-13,16,20H,4-5,8,14-15,17H2,1-3H3,(H,29,30,35)/b11-7+/t20-/m1/s1
Canonical SMILES:
CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2C4CCCCN(C4)C(=O)C=CCN(C)C)C(=CC=C3)Cl
1.Optimal management of EGFR-mutant non-small cell lung cancer with disease progression on first-line tyrosine kinase inhibitor therapy.
Liao BC;Lin CC;Lee JH;Yang JC Lung Cancer. 2017 Aug;110:7-13. doi: 10.1016/j.lungcan.2017.05.009. Epub 2017 May 11.
The first-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs), gefitinib and erlotinib, and the second-generation EGFR-TKI, afatinib, have all been approved as standard first-line treatments for advanced EGFR-mutant non-small cell lung cancer (NSCLC) based on superior progression-free survival results compared to platinum doublet chemotherapy regimens. Acquired resistance to an EGFR-TKI inevitably develops after a period of effective drug treatment. After tumor progression, many combination therapy regimens that include an EGFR-TKI, or EGFR-TKI monotherapy, have been tested in prospective trials with the aim of extending survival. Third-generation EGFR-TKIs such as osimertinib have been developed with the aim of overcoming the effects of EGFR T790M resistance mutation, which occurs in half of the patients with disease progression on EGFR-TKI therapy. Osimertinib has become the standard treatment in patients for whom tumor re-biopsy reveals an acquired EGFR T790M mutation following EGFR-TKI therapy. Other third-generation EGFR-TKIs, such as olmutinib, EGF816, and ASP8273, are still in the trial phase.
2.Update on recent preclinical and clinical studies of T790M mutant-specific irreversible epidermal growth factor receptor tyrosine kinase inhibitors.
Liao BC;Lin CC;Lee JH;Yang JC J Biomed Sci. 2016 Dec 3;23(1):86.
The first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors (1/2G EGFR-TKIs) gefitinib, erlotinib, and afatinib have all been approved as standard first-line treatments for advanced EGFR mutation-positive non-small cell lung cancer. The third-generation (3G) EGFR-TKIs have been developed to overcome the EGFR T790M mutation, which is the most common mechanism of acquired resistance to 1/2G EGFR-TKI treatment. This resistance mutation develops in half of the patients who respond to 1/2G EGFR-TKI therapy. The structures of the novel 3G EGFR-TKIs are different from those of 1/2G EGFR-TKIs. Particularly, 3G EGFR-TKIs have lower affinity to wild-type EGFR, and are therefore associated with lower rates of skin and gastrointestinal toxicities. However, many of the adverse events (AEs) that are observed in patients receiving 3G EGFR-TKIs have not been observed in patients receiving 1/2G EGFR-TKIs. Although preclinical studies have revealed many possible mechanisms for these AEs, the causes of some AEs remain unknown. Many mechanisms of resistance to 3G EGFR-TKI therapy have also been reported. Here, we have reviewed the recent clinical and preclinical developments related to novel 3G EGFR-TKIs, including osimertinib, rociletinib, olmutinib, EGF816, and ASP8273.
3.Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance.
Patel H;Pawara R;Ansari A;Surana S Eur J Med Chem. 2017 Dec 15;142:32-47. doi: 10.1016/j.ejmech.2017.05.027. Epub 2017 May 11.
EGFR T790M mutation leads to resistance to most of clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development, which includes osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. On the other hand recently EGFR C797S mutation was reported to be a leading mechanism of resistance to the third-generation inhibitors. The C797S mutation appears to be an ideal target for overcoming the acquired resistance to the third generation inhibitors. This review summarizes the third generation inhibitors, synthesis, their mechanism of resistance and latest development on the discovery of a fourth-generation EGFR TKIs and U to Y allosteric strategies to combat the C797S EGFR resistance problem.
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CAS 1508250-71-2 EGF816

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