1909226-00-1 Usage
Biological Activity
bda-366 is a selective antagonist of bcl2 bh4 domain with ki value of 3.3 nm [1].bcl2 is an important anti-apoptotic protein. bcl2 homology 4 (bh4) domain is required for its antiapoptotic function, thus acts as a promising anticancer target [1].bda-366 is a selective bcl2 inhibitor. bda-366 induced conformational change of bcl2 that exposed the bh3 domain, resulting in abrogation of its prosurvival function and conversion of bcl2 to a prodeath protein. in non-small cell lung cancer (nsclc) and small cell lung cancer (sclc) cells, bda-366 selectively bound to bcl2 with high affinity. bda-366 induced apoptosis by bcl2-dependent bax activation and cytochrome c release. in h460 cells, bda-366 reduced bcl2/ip3r binding, which then increased ca2+ release [1].in mice bearing h460 lung cancer xenografts, treatment with bda-366 (0, 10, 20, and 30 mg/kg/day) via i.p. route for 14 days induced apoptosis and potently inhibited tumor growth in a dose-dependent way. there was no significant toxicity at the maximum therapeutic dose. in tumor tissue from patients with nsclc, bda-366 synergized with rad001 and resulted in significantly greater inhibition of lung cancer growth compared with either agent alone [1].
references
[1]. han b, park d, li r, et al. small-molecule bcl2 bh4 antagonist for lung cancer therapy. cancer cell, 2015, 27(6): 852-863.
Check Digit Verification of cas no
The CAS Registry Mumber 1909226-00-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,9,0,9,2,2 and 6 respectively; the second part has 2 digits, 0 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1909226-00:
(9*1)+(8*9)+(7*0)+(6*9)+(5*2)+(4*2)+(3*6)+(2*0)+(1*0)=171
171 % 10 = 1
So 1909226-00-1 is a valid CAS Registry Number.
1909226-00-1Relevant academic research and scientific papers
Jiang, Jack B.,Johnson, Mary George,Defauw, Jean M.,Beine, Tracey M.,Ballas, Lawrence M.,et al.
, p. 4259 - 4263 (1992)
A novel series od diaminoanthraquinones was discovered initially as protein kinase C inhibitors with IC50s in the 50-100 μM range.They exhibited potent tumor cell growth inhibitory activity in vitro without cross resistance to adriamycin.Further evaluation of two of the most active compounds NSC 639365 (3) and NSC 639366 (4) in human tumor cloning assay showed potent cytocidal activity.The results suggest therapeutical potentials against human tumors.
