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ChemicalBook--->CAS DataBase List--->934343-74-5

934343-74-5

934343-74-5 Structure

934343-74-5 Structure
IdentificationBack Directory
[Name]

NVP-HSP990(HSP990)
[CAS]

934343-74-5
[Synonyms]

CS-786
HSP-990
NVP-HSP990
NVP-HSP990(HSP990)
HSP990 (NVP-HSP990)
NVP-HSP990(HSP990) USP/EP/BP
(7R)-2-Amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d
(R)-2-Amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one
(R)-2-Amino-7-(4-fluoro-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one
(7R)-2-AMINO-7-[4-FLUORO-2-(6-METHOXYPYRIDIN-2-YL)PHENYL]-4-METHYL-7,8-DIHYDRO-6H-PYRIDO[4,3-D]PYRIMIDIN-5-ONE
(7R)-2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-pyrido[4,3-d]pyrimidin-5(6H)-one
Pyrido[4,3-d]pyrimidin-5(6H)-one, 2-amino-7-[4-fluoro-2-(6-methoxy-2-pyridinyl)phenyl]-7,8-dihydro-4-methyl-, (7R)-
[Molecular Formula]

C20H18FN5O2
[MDL Number]

MFCD22628859
[MOL File]

934343-74-5.mol
[Molecular Weight]

379.39
Chemical PropertiesBack Directory
[density ]

1.332
[storage temp. ]

Store at -20°C
[solubility ]

insoluble in H2O; insoluble in EtOH; ≥12.3 mg/mL in DMSO
[form ]

solid
[color ]

Off-white to yellow
Safety DataBack Directory
[HS Code ]

29339900
Hazard InformationBack Directory
[Uses]

NVP-HSP990 is an orally available HSP90 inhibitor.
[Biological Activity]

hsp990 (nvp-hsp990) is a potent and selective inhibitor of hsp90 with ic50 values of 0.6, 0.8 and 8.5 nm for hsp90α, hsp90β and grp94, respectively [1].heat shock protein 90 (hsp90) is a chaperone protein that stabilizes proteins against heat stress, assists proteins to fold properly and aids in protein degradation. also, hsp90 stabilizes proteins required for tumor growth.hsp990 (nvp-hsp990) is a potent and selective hsp90 inhibitor. nvp-hsp990 bound to the n-terminal atp-binding domain of hsp90. nvp-hsp990 inhibited trap1 atpase activity by 90% with ic50 value of 320 nm. in gtl-16 cells, nvp-hsp990 destabilized the hsp90-p23 complex in a concentration- and time-dependent way. also, nvp-hsp990 decreased c-met with ec50 value of 37 nm and induced hsp70 with ec50 value of 20 nm. nvp-hsp990 inhibited erk and akt phosphorylation with ec50 values of 11 and 6 nm respectively and thus inhibited erk and akt activation. in five human tumor cell lines, nvp-hsp990 inhibited cell growth with gi50 values of 4-40 nm [1]. in glioma tumor-initiating cells, nvp-hsp990 inhibited cell growth with ic50 value of 10-500 nm in a dose-dependent way and reduced cdk2 and cdk4, thus disrupting cell-cycle control [2].in the gtl-16 gastric cancer mice model, nvp-hsp990 exhibited antitumor efficacy [1].
[storage]

Store at -20°C
[References]

[1]. menezes dl, taverna p, jensen mr, et al. the novel oral hsp90 inhibitor nvp-hsp990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. mol cancer ther, 2012, 11(3): 730-739.
[2]. fu j, koul d, yao j, et al. novel hsp90 inhibitor nvp-hsp990 targets cell-cycle regulators to ablate olig2-positive glioma tumor-initiating cells. cancer res, 2013, 73(10): 3062-3074.
Spectrum DetailBack Directory
[Spectrum Detail]

NVP-HSP990(HSP990)(934343-74-5)1HNMR
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