Aurora A Inhibitor I

Bezeichnung:Aurora A Inhibitor I

CAS-Nr1158838-45-9

Englisch Name:Aurora A Inhibitor I

CBNumberCB62506281

SummenformelC31H31ClFN7O2

Molgewicht588.07

MOL-Datei1158838-45-9.mol

Aurora A Inhibitor I physikalisch-chemischer Eigenschaften

Dichte	1.362
storage temp.	2-8°C
Löslichkeit	DMSO: soluble10mg/mL, clear
Aggregatzustand	powder
Farbe	white to beige
InChIKey	AKSIZPIFQAYJGF-UHFFFAOYSA-N

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3

Gefahreninformationscode (GHS)

Aurora A Inhibitor I Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
TC-S 7010 is a selective Aurora A inhibitor.
Definition
ChEBI: N-(2-chlorophenyl)-4-[[2-[4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]anilino]-5-fluoro-4-pyrimidinyl]amino]benzamide is a member of benzamides.
Biologische Aktivität
aurora a inhibitor i is a novel, potent, and selective inhibitor of aurora a .aurora kinases are reported to be required for mitosis and to complete cell division. because of this, aurora kinase inhibitors have been investigated extensively as potential anticancer therapeutic agents. the two major aurora kinases (aurora a and aurora b) are closely related in kinase domain sequence (71% identical).
in vitro
aurora a inhibitor i was tested against wild-type kinase and two mutants (aurora a (t217e) and aurora b (e161t)). the inhibitory potencies of aurora a inhibitor i was strongly affected by the single amino acid substitutions. for either aurora kinase, the presence of threonine allowed potent inhibition, while for glutamic acid variants, there was a approximately 100-fold shift in ic50, which supported the “gating” role for this residue. the aurora b binding pocket was enlarged by the e161t mutation, while the pocket in aurora a was closed by the t217e mutation. aurora a inhibitor i was exceptionally selective aurora a inhibitors, as shown by no inhibition on aurora b or cdks was observed in cellular assays [1].
IC 50
3.4 nm.
Lager
Store at +4°C
Einzelnachweise
[1] aliagas-martin i,burdick d,corson l,dotson j,drummond j,fields c,huang ow,hunsaker t,kleinheinz t,krueger e,liang j,moffat j,phillips g,pulk r,rawson te,ultsch m,walker l,wiesmann c,zhang b,zhu by,cochran ag. a class of 2,4-bisanilinopyrimidine aurora a inhibitors with unusually high selectivity against aurora b. j med chem.2009 may 28;52(10):3300-7.

Aurora A Inhibitor I Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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