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| | NVP-HSP990(HSP990) Basic information |
| Product Name: | NVP-HSP990(HSP990) | | Synonyms: | CS-786;NVP-HSP990(HSP990);HSP-990;NVP-HSP990;(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;(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;HSP990 (NVP-HSP990);(7R)-2-Amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d | | CAS: | 934343-74-5 | | MF: | C20H18FN5O2 | | MW: | 379.39 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 934343-74-5.mol |  |
| | NVP-HSP990(HSP990) Chemical Properties |
| density | 1.332 | | storage temp. | Store at -20°C | | solubility | insoluble in H2O; insoluble in EtOH; ≥12.3 mg/mL in DMSO | | form | solid |
| | NVP-HSP990(HSP990) Usage And Synthesis |
| 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]. | | 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. |
| | NVP-HSP990(HSP990) Preparation Products And Raw materials |
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