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1508250-72-3 (EGF816 (mesylate))

1

Identification

EGF816 (mesylate) EGF816 (mesylate)
Name EGF816 (mesylate)
Formula C27H35ClN6O5S
MW 591.12
CAS No. 1508250-72-3
EINECS
Smiles O=C(C1=CC(C)=NC=C1)NC2=NC3=CC=CC(Cl)=C3N2[[email protected]]4CN(C(/C=C/CN(C)C)=O)CCCC4.CS(=O)(O)=O
Synonyms EGF-816 mesylate;Nazartinib mesylate; (R,E)-N-(7-chloro-1-(1-(4-(dimethylamino)but-2-enoyl)azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide methanesulfonate
InChI InChI=1S/C26H31ClN6O2.CH4O3S/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)/b11-7+;/t20-;/m1./s1
2

Introduction

EGF816 mesylate is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC.

Background Information

EGF816 mesylate is the mesylate salt of EGF816 which is a covalent mutant-selective EGFR inhibitor and potently inhibits the T790M. ......by BOC Sciences
EGF816 mesylate is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000070546

Storage condition

Solubility

No data available by CHEMSCENE, LLC
No data available by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer
Indications Non Small Cell Lung Cancer
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
EGF816 (mesylate) Novartis Pharmaceuticals Non Small Cell Lung Cancer 2014/12/18 Phase 2
EGF816 (mesylate) - Not Found
EGF816 (mesylate) - No Development Reported
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Safety Data of EGF816 (mesylate)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD420();10mg/USD600() USA
MedChemexpress Co., Ltd. 5mg/USD420();10mg/USD600() USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD420();10mg/USD600() China
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Related Products

Other Forms of 1508250-72-3

Name CAS No Formula MW
EGF816 (S-enantiomer) 1508256-20-9 C26H31ClN6O2 495.0163
EGF816 1508250-71-2 C26H31ClN6O2 495.02

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD168393 194423-15-9 C17H13BrN4O 369.2153
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanol 481-74-3 C15H10O4 254.2375
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
EGF816 1508250-71-2 C26H31ClN6O2 495.02
AZD-9291 1421373-65-0 C28H33N7O2 499.61
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Route of Synthesis

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References

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More Information

EGF816 (mesylate)

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