CYD-2-11

Research use only, not for human use.

CYD-2-11 is a novel potent, selective Bax agonist that targets the structural pocket proximal to S184 in the C-terminal region of Bax (Ki=34.1 nM).

CYD-2-11 is a novel potent, selective Bax agonist that targets the structural pocket proximal to S184 in the C-terminal region of Bax (Ki=34.1 nM); shows no affinity for other Bcl-2 family members; directly activates Bax proapoptotic activity by inducing a conformational change enabling formation of Bax homooligomers in mitochondrial membranes; suppresses malignant growth without evident significant toxicity to normal tissues in mutant KRAS-driven lung cancer models; displays strong synergistic activity and overcomes rapalog resistance combined with RAD001.

CYD-2-11 (0-100 μM; 48 h) shows anti-proliferation effects to breast cancer cells.CYD-2-11 (5 μM; 48 h) selectively binds to Bax protein and induces apoptosis in NSCLC and SCLC cell lines. Cell Proliferation Assay Cell Line:T47D, MCF-7, MDA-MB-231, MDA-MB-468 and MCF-10A cell lines Concentration:0.01, 0.1, 1, 5, 10 and 100 μM Incubation Time:48 hours Result:Inhibited cell proliferation of T47D, MCF-7, MDA-MB-231, MDA-MB-468 and MCF-10A cells with IC50 values of 4.37, 9.47, 3.81, 3.22 and 8.73 μM, respectively.Apoptosis Analysis Cell Line:SCLC and NSCLC cell lines Concentration:5 μM Incubation Time:48 hours Result:Induced cell apoptosis in both SCLC and NSCLC cells with a higher effect than SMBA1.

CYD-2-11 (20 mg/kg; i.p.; once daily for 7 days) inhibits tumor growth.CYD-2-11 (40 mg/kg; i.p.; once daily for 14 days) represses lung cancer growth and overcomes rapalog resistance with the combination of RAD001 (1 mg/kg) in murine lung cancer models. Animal Model:Female nude mice with MDA-MB-231 tumor xenografts Dosage:20 mg/kg Administration:Intraperitoneal injection; 20 mg/kg; once daily for 7 days Result:Exhibited a 57% inhibition rate of MDA-MB-231 tumor growth in vivo.

CYD-2-11 | CYD 2 11 | CYD211

Angiogenesis

Bcl-2

Bcl-2

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1425944-22-4

358.397

C22H18N2O3

>98% (HPLC)

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NCCOC1=CC=CC=C1/C=C2C3=C(C4=C/2C=CC=C4)C=CC([N+]([O-])=O)=C3

(E)-2-(2-((2-nitro-9H-fluoren-9-ylidene)methyl)phenoxy)ethan-1-amine

(-20℃)

With Ice Pack

≥ 2 years