MYCMI-6
- CAS号:681282-09-7
- 英文名:MYCMI-6
- 中文名:MYCMI-6
- CBNumber:CB84668251
- 分子式:C20H19N7O
- 分子量:373.41
- MOL File:681282-09-7.mol
- 沸点 :699.5±55.0 °C(Predicted)
- 密度 :1.46±0.1 g/cm3(Predicted)
- 储存条件 :under inert gas (nitrogen or Argon) at 2–8 °C
- 酸度系数(pKa) :7.53±0.10(Predicted)
- 形态 :Solid
- 颜色 :Brown to reddish brown
MYCMI-6性质、用途与生产工艺
- 生物活性 MYCMI-6 (NSC354961) 是一种有效的选择性内源性 MYC:MAX 蛋白相互作用抑制剂。 MYCMI-6 阻断 MYC 驱动的转录。MYCMI-6 选择性结合 MYC bHLHZip 域,Kd 值为 1.6 μM。MYCMI-6 以 MYC 依赖性的方式抑制肿瘤细胞的生长 (IC50<0.5 μM)。MYCMI-6 对正常人细胞无细胞毒性。MYCMI-6 诱导细胞凋亡 (apoptosis)。
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体外研究
MYCMI-6 (NSC354961) (6.25 μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy.
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations of MYC to one of the immunoglobulin loci - in a dose-dependent manner with an average GI 50 of 0.5 μM. Treatment of MCF7 cells with the MYCMI-6 for 24 hours significantly decreased MYC:MAX isPLA signals to 7%. Titration showed an IC 50 for inhibition of MYC:MAX of less than 1.5 μM for MYCMI-6 by isPLA. MYCMI-6 inhibits the MYC:MAX heterodimer formation with an IC 50 of 3.8 μM. MYCMI-6 efficiently inhibits anchorage-independent growth of MYCN -amplified neuroblastoma cells with GI 50 values of <0.4 μM.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. -
体内研究
MYCMI-6 (20 mg/kg; i.p.; daily for 1-2 weeks) induces massive apoptosis and reduces tumor cell proliferation, tumor microvasculature density and MYC:MAX interaction in a MYC-dependent xenograft tumor model.
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.
- 更新日期:2024/08/19
- 产品编号:HY-124675
- 产品名称:MYCMI-6 MYCMI-6
- CAS编号:681282-09-7
- 包装:5mg
- 价格:800元
- 更新日期:2024/08/19
- 产品编号:HY-124675
- 产品名称:MYCMI-6 MYCMI-6
- CAS编号:681282-09-7
- 包装:10 mg
- 价格:1120元
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:19892
- 优势度:58
- 公司名称:BOC Sciences
- 联系电话:+1-631-485-4226
- 电子邮件:inquiry@bocsci.com
- 国家:美国
- 产品数:19553
- 优势度:58
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58