WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H414006
CAS#: 1784778-10-4 (mesylate hydrate)
Description: Nazartinib mesylate trihydrate is an antineoplastic
Hodoodo Cat#: H414006
Name: Nazartinib mesylate trihydrate
CAS#: 1784778-10-4 (mesylate hydrate)
Chemical Formula: C27H41ClN6O8S
Exact Mass: 644.24
Molecular Weight: 645.170
Elemental Analysis: C, 50.27; H, 6.41; Cl, 5.49; N, 13.03; O, 19.84; S, 4.97
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Related CAS #: 1784778-10-4 (mesylate hydrate) 1508250-72-3 (mesylate) 1508250-71-2 (free base)
Synonym: Nazartinib mesylate; EGF816 mesylate trihydrate; EGF 816 mesylate trihydrate; EGF-816 mesylate trihydrate
IUPAC/Chemical Name: (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide methanesulfonate trihydrate
InChi Key: HCKBCMVQGLVGEA-ZBFDXWMPSA-N
InChi Code: InChI=1S/C26H31ClN6O2.CH4O3S.3H2O/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;1-5(2,3)4;;;/h6-7,9-13,16,20H,4-5,8,14-15,17H2,1-3H3,(H,29,30,35);1H3,(H,2,3,4);3*1H2/b11-7+;;;;/t20-;;;;/m1..../s1
SMILES Code: CN(C/C=C/C(N1CCCC[C@@H](n(c(NC(c2cc(C)ncc2)=O)n3)c4c3cccc4Cl)C1)=O)C.CS(=O)(O)=O.O.O.O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 645.17 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Jia Y, Juarez J, Li J, Manuia M, Niederst MJ, Tompkins C, Timple N, Vaillancourt MT, Pferdekamper AC, Lockerman EL, Li C, Anderson J, Costa C, Liao D, Murphy E, DiDonato M, Bursulaya B, Lelais G, Barretina J, McNeill M, Epple R, Marsilje TH, Pathan N, Engelman JA, Michellys PY, McNamara P, Harris J, Bender S, Kasibhatla S. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602. doi: 10.1158/0008-5472.CAN-15-2581. PubMed PMID: 26825170.
2: Lelais G, Epple R, Marsilje TH, Long YO, McNeill M, Chen B, Lu W, Anumolu J, Badiger S, Bursulaya B, DiDonato M, Fong R, Juarez J, Li J, Manuia M, Mason DE, Gordon P, Groessl T, Johnson K, Jia Y, Kasibhatla S, Li C, Isbell J, Spraggon G, Bender S, Michellys PY. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imid azol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers. J Med Chem. 2016 Jul 28;59(14):6671-89. doi: 10.1021/acs.jmedchem.5b01985. PubMed PMID: 27433829.
3: Liao BC, Lin CC, Lee JH, Yang JC. Update on recent preclinical and clinical studies of T790M mutant-specific irreversible epidermal growth factor receptor tyrosine kinase inhibitors. J Biomed Sci. 2016 Dec 3;23(1):86. Review. PubMed PMID: 27912760; PubMed Central PMCID: PMC5135794.
4: Wang S, Cang S, Liu D. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z. Review. PubMed PMID: 27071706; PubMed Central PMCID: PMC4830020.
5: Sun JM, Park K. Can we define the optimal sequence of epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of epidermal growth factor receptor-mutant nonsmall cell lung cancer? Curr Opin Oncol. 2017 Mar;29(2):89-96. doi: 10.1097/CCO.0000000000000350. PubMed PMID: 28085680.
6: Kobayashi Y, Mitsudomi T. Not all epidermal growth factor receptor mutations in lung cancer are created equal: Perspectives for individualized treatment strategy. Cancer Sci. 2016 Sep;107(9):1179-86. doi: 10.1111/cas.12996. Review. PubMed PMID: 27323238; PubMed Central PMCID: PMC5021039.
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