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NU 2058

NU 2058 ??? ???
?? ??:
161058-83-9
???:
NU 2058
???(??):
CS-2601;NU2058>2-aMino-6-purine;NU2058, 10 mM in DMSO;NU 2058;NU-2058;NU2058;O-Cyclohexylmethylguanine;2-Amino-6-(cyclohexylmethoxy)purine;NU-2058;O6-(CYCLOHEXYLMETHYL)GUANINE;6-(Cyclohexylmethoxy)-9H-purin-2-amine;2-aMino-6-[(cyclohexylMethyl)oxy]purine
CBNumber:
CB4498289
???:
C12H17N5O
??? ??:
247.3
MOL ??:
161058-83-9.mol
MSDS ??:
SDS

NU 2058 ??

???
199°C(lit.)
?? ?
424.8±55.0 °C(Predicted)
??
1.52±0.1 g/cm3(Predicted)
?? ??
Keep in dark place,Sealed in dry,2-8°C
???
DMSO: 22mg/mL
??? ??
powder to crystal
?? ?? (pKa)
7.36±0.20(Predicted)
??
???
?? ??(λmax)
281nm(MeOH)(lit.)
InChIKey
MWGXGTJJAOZBNW-UHFFFAOYSA-N
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
??? ?? Xi
?? ???? ?? 36/37/38
????? 26-36/37
WGK ?? 3
HS ?? 2933.99.9000
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P261 ??·?·??·???·??·...·????? ??? ????.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P271 ?? ?? ??? ? ?? ???? ?????.
P280 ????/???/???/?????? ?????.
P302+P352 ??? ??? ??? ?? ????.
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
NFPA 704
0
2 0

NU 2058 C??? ??, ??, ??

??

NU 2058 is an inhibitor of cyclin-dependent kinase 1 (Cdk1) and Cdk2 (IC50s = 7.0 and 17 μM, respectively). Increased Cdk activity is often associated with human tumors, and inhibitors of Cdks, including NU 2058, can arrest cell cycling in cancer cells in vitro.

??

NU 2058 is an intermediate of NU 6140 (N925295), a cyclin-dependant kinase 2 inhibitor which demonstrates 10-36 fold selectivity against Cdk2-cyclin A. This selectivity induces cell-cycle arrest at the G2-M phase and potentiates the apoptotic effect of pacitaxel.

???? ??

Cyclin-dependent kinase (cdk) 1 and cdk2 inhibitor (K i values are 5 and 12 μ M respectively). Inhibits growth of human tumor cells in vitro (mean GI 50 = 13 μ M). Also inhibits DNA topoisomerase II ATPase activity (IC 50 = 300 μ M).

NU 2058 ?? ?? ? ???

???

?? ??

NU 2058 ?? ??

???( 99)?? ??
??? ?? ??? ?? ?? ? ??
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NU 2058 ?? ??:

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