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ChemicalBook--->CAS DataBase List--->807640-87-5

807640-87-5

807640-87-5 Structure

807640-87-5 Structure
IdentificationBack Directory
[Name]

JNJ 26483327
[CAS]

807640-87-5
[Synonyms]

BGB102
BGB-102
BGB 102
MTKi-327
EOS-60486
JNJ26483327
JNJ-26483327
JNJ 26483327
BGB102,BGB 102
17-Bromo-1,8,9,10,11,12,13,14-octahydro-20-methoxy-13-methyl-4,6-ethenopyrimido[4,5-b][6,1,12]benzoxadiazacyclopentadecine
4,6-Ethenopyrimido[4,5-b][6,1,12]benzoxadiazacyclopentadecine, 17-bromo-1,8,9,10,11,12,13,14-octahydro-20-methoxy-13-methyl-
[Molecular Formula]

C22H25BrN4O2
[MDL Number]

MFCD28386291
[MOL File]

807640-87-5.mol
[Molecular Weight]

457.36
Chemical PropertiesBack Directory
[Boiling point ]

582.4±50.0 °C(Predicted)
[density ]

1.310±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

8.26±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
[in vivo]

JNJ-26483327 (75 mg/kg, p.o.) delays xenograft tumour growth compared to vehicle treatment, but when combines with Herceptin, they can abrogate the PKB feedback loop and is synergistic in inhibition of xenograft tumour growth[1].

[IC 50]

EGFR: 9.6 nM (IC50); HER2: 18 nM (IC50); HER4: 40.3 nM (IC50)
[References]

[1] Gijsen M, et al. HER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 herceptin in breast cancer. PLoS Biol. 2010 Dec 21;8(12):e1000563. DOI:10.1371/journal.pbio.1000563
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