MYCMI-6

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MYCMI-6 (NSC354961) 是一种选择性、高亲和力的 MYC-MAX 相互作用抑制剂。

MYCMI-6 (NSC354961) is a selective, high affinity inhibitor of MYC-MAX interaction, blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with Kd of 1.6 uM in SPR assay; specifcally targets MYC:MAX interaction without interfering with other MYC activities, selectively suppresses MYC-driven tumor cell growth with high efficacy, efficiently inhibits anchorage-independent growth of MYCN-amplifed neuroblastoma cells with GI50 values of <0.4, 5 and 0.75 μM, respectively; reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects

Cell Viability Assay Cell Line:MYCN-amplified neuroblastoma cells (IMR-32, Kelly and SK-N-DZ), MYCN-non-amplified neuroblastoma cells (SK-N-F1, SK-N-AS and SK-N-RA)Concentration:6.25?μM Incubation Time:48 hours Result:Reduced growth of the MYCN-amplified cell lines significantly stronger than the MYCN-non-amplified cell lines.

Animal Model:6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells) Dosage:20?mg/kg body weight Administration:I.p.; daily for 1-2 weeks Result:A dramatic increase in the extension of apoptotic areas in the tumors and a significant increase in non-proliferative areas as determined by Ki67 staining in tumors.

NSC354961 | MYCMI6

Cell Cycle/DNA Damage

c-Myc

c-Myc

——

——

681282-09-7

373.42

C20H19N7O

>98% (HPLC)

In Vitro:?DMSO : 2.4 mg/mL (6.43 mM)

CCOC1=CC2=C(C3=C(C=C(C=C3)N=NC4=C(N=C(C=C4)N)N)N=C2C=C1)N

(E)-3-((9-amino-7-ethoxyacridin-3-yl)diazenyl)pyridine-2,6-diamine

(-20℃)

With Ice Pack

≥ 2 years