EGF816 mesylate
CAS No. 1508250-72-3
EGF816 mesylate ( EGF-816 mesylate;Nazartinib mesylate )
Catalog No. M12106 CAS No. 1508250-72-3
EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
Size | Price / USD | Stock | Quantity |
5MG | 873 | Get Quote |
|
50MG | 1782 | Get Quote |
|
100MG | 2250 | Get Quote |
|
200MG | Get Quote | Get Quote |
|
500MG | Get Quote | Get Quote |
|
1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameEGF816 mesylate
-
NoteResearch use only, not for human use.
-
Brief DescriptionEGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.
-
DescriptionEGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively; shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 of 5, 1, and 3 nM, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively, inhibitscell proliferation with EC50 of 9, 11, and 25 nM, but not the WT EGFR-containing patient-derived cell lines; potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro; causes tumor regressions in vivo in several patient-derived xenograft models, also demonstrates antitumor activity in exon 20 insertion mutant model.Lung Cancer Phase 3 Clinical
-
SynonymsEGF-816 mesylate;Nazartinib mesylate
-
PathwayAngiogenesis
-
TargetEGFR
-
RecptorEGFR
-
Research AreaCancer
-
IndicationLung Cancer
Chemical Information
-
CAS Number1508250-72-3
-
Formula Weight591.12
-
Molecular FormulaC27H35ClN6O5S
-
Purity>98% (HPLC)
-
Solubility10 mM in DMSO
-
SMILESCC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2C4CCCCN(C4)C(=O)C=CCN(C)C)C(=CC=C3)Cl.CS(=O)(=O)O
-
Chemical Name4-Pyridinecarboxamide, N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-, methanesulfonate (1:1)
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Lelais G, et al. J Med Chem. 2016 Jul 28;59(14):6671-89.
2. Jia Y, et al. Cancer Res. 2016 Mar 15;76(6):1591-602.
3. Liao BC, et al. Lung Cancer. 2017 Aug;110:7-13.
2. Jia Y, et al. Cancer Res. 2016 Mar 15;76(6):1591-602.
3. Liao BC, et al. Lung Cancer. 2017 Aug;110:7-13.
molnova catalog
related products
-
Poziotinib hydrochlo...
Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors.?It is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.?
-
TX1-85-1
TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
-
(1R,2R)-Trans-N-Boc-...
Cyclohexanediamine has a potential of anticancer activity.