A 366

Name	5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
Synonyms	A 366 A-366 A-336 A366 CS-2077 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine Spiro[cyclobutane-1,3'-[3H]indol]-2'-amine, 5'-methoxy-6'-[3-(1-pyrrolidinyl)propoxy]-
CAS	1527503-11-2
EINECS	808-907-0

UN IDs	UN 3077 9 / PGIII
WGK Germany	3

Last Update：2024-01-02 23:10:35

biological activity	A-366 is a highly efficient and selective peptide competitive histone methyltransferase G9a inhibitor, the IC50 for G9a and GLP were 3.3 and 38 nM, respectively. A- 366 was 1000 times more selective than the other 21 methyltransferases. A- 366 was A potent inhibitor of the Spindlin1-H3K4me3 interaction (IC50=182.6 nM). A- 366 exhibits high affinity for human H3R (Ki = 17 nM) and subtype selectivity across subpopulations of the histaminergic and dopaminergic receptor families.
Cell Line:	MV4;11 cells
Concentration:	0.01-10 μM
Incubation Time:	14 days
Result:	Resulted in inhibited proliferation and a decrease in viability corresponding to the dose response observed for CD11b staining. A modest 45% tumor growth inhibition resulting from A-366 treatment in this model.
Animal Model:	6-8 week old SCID-beige female mice (MV4;11 xenografts)
Dosage:	30 mg/kg
Administration:	By osmotic mini-pump; daily for 14 days