MYCMI-6
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- CAS号:
- 681282-09-7
- 英文名:
- MYCMI-6
- 英文别名:
- MYCMI-6;NSC354961;MYCMI-6(NSC 354961);3-((9-Amino-7-ethoxyacridin-3-yl)diazenyl)pyridine-2,6-diamine;2,6-Pyridinediamine, 3-[2-(9-amino-7-ethoxy-3-acridinyl)diazenyl]-;NSC 354961,cells,neuroblastoma,cytotoxic,mice,tumor,inhibit,nude,lymphoma,MYCMI-6,athymic,Inhibitor,NSC-354961,MYC-driven,Apoptosis,Myc,c-Myc,MYCMI6,MCF7,MYCMI 6
- 中文名:
- MYCMI-6
- 中文别名:
- 化合物MYCMI-6;3-((9-氨基-7-乙氧基吖啶-3-基)偶氮基)吡啶-2,6-二胺
- CBNumber:
- CB84668251
- 分子式:
- C20H19N7O
- 分子量:
- 373.41
- MOL File:
- 681282-09-7.mol
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MYCMI-6化学性质
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沸点:
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699.5±55.0 °C(Predicted)
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密度:
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1.46±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2–8 °C
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酸度系数(pKa):
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7.53±0.10(Predicted)
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MYCMI-6性质、用途与生产工艺
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)。
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:
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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)
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Concentration:
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6.25 μM
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Incubation Time:
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48 hours
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Result:
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Reduced growth of the
MYCN
-amplified cell lines significantly stronger than the
MYCN
-non-amplified cell lines.
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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:
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6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells)
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Dosage:
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20 mg/kg body weight
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Administration:
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I.p.; daily for 1-2 weeks
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Result:
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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.
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MYCMI-6
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-124675 | MYCMI-6 MYCMI-6 | 681282-09-7 | 5mg | 800元 |
2024/04/30 | HY-124675 | MYCMI-6 MYCMI-6 | 681282-09-7 | 10 mg | 1120元 |
681282-09-7, MYCMI-6 相关搜索:
- 化合物MYCMI-6
- 3-((9-氨基-7-乙氧基吖啶-3-基)偶氮基)吡啶-2,6-二胺
- 681282-09-7
- NSC 354961,cells,neuroblastoma,cytotoxic,mice,tumor,inhibit,nude,lymphoma,MYCMI-6,athymic,Inhibitor,NSC-354961,MYC-driven,Apoptosis,Myc,c-Myc,MYCMI6,MCF7,MYCMI 6
- 3-((9-Amino-7-ethoxyacridin-3-yl)diazenyl)pyridine-2,6-diamine
- MYCMI-6(NSC 354961)
- 2,6-Pyridinediamine, 3-[2-(9-amino-7-ethoxy-3-acridinyl)diazenyl]-
- NSC354961
- MYCMI-6