1202916-90-2 Usage
Uses
CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.
Biological Activity
pim kinases (provirus integration site for moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. this family of kinases is composed of three different isoforms (pim-1, pim-2, and pim-3). the simultaneous inhibition of pim-1, pim-2, and pim-3 kinases is emerging as a promising strategy for anticancer drug development. cx-6258 is a potent, selective, and orally efficacious pan-pim kinases inhibitor.
in vitro
cx-6258 exhibited in vitro synergy with chemotherapeutics. the antiproliferative activity of cx-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. cx-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].
in vivo
cx-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia mv-4-11, and prostate adenocarcinoma pc3. the drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (tgi) and a 100 mg/kg dose producing 75% tgi. in addition, cx-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where pim kinases had been shown to play an important role [1].
references
[1] haddach m, michaux j, schwaebe mk, et al. discovery of cx-6258. a potent, selective, and orally efficacious pan-pim kinases inhibitor. acs med chem lett. 2011;3(2):135-9.
Check Digit Verification of cas no
The CAS Registry Mumber 1202916-90-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,2,9,1 and 6 respectively; the second part has 2 digits, 9 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1202916-90:
(9*1)+(8*2)+(7*0)+(6*2)+(5*9)+(4*1)+(3*6)+(2*9)+(1*0)=122
122 % 10 = 2
So 1202916-90-2 is a valid CAS Registry Number.
1202916-90-2Relevant articles and documents
Synthesis of [11C]CX-6258 as a new PET tracer for imaging of Pim kinases in cancer
Wang, Min,Tzintzun, Reynaldo,Gao, Mingzhang,Xu, Zhidong,Zheng, Qi-Huang
, p. 3831 - 3835 (2015/08/24)
Abstract The reference standard CX-6258 {(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, 4a} and its desmethylated precursor N-desmethyl-CX-6258 {(E)-3-((5-(3-(1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)-5-chloroindolin-2-one, 5} for radiolabeling were synthesized from 5-bromo-2-furaldehyde and 3-carboxybenzeneboronic acid in 3 and 4 steps with 29-49% and 24-32% overall chemical yield, respectively. The target tracer [11C]CX-6258 {(E)-5-chloro-3-((5-(3-(4-[11C]methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, [11C]4a} was prepared from N-desmethyl-CX-6258 (5) with [11C]CH3OTf under basic condition (2 N NaOH) through N-[11C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 40-50% radiochemical yield based on [11C]CO2 and decay corrected to end of bombardment (EOB) with 370-1110 GBq/μmol specific activity at EOB.
OXINDOLE COMPOUNDS
-
Page/Page column 105-106, (2010/03/04)
The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.
