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MYCMI-6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MYCMI-6图片
CAS NO:681282-09-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
NSC354961
产品介绍
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)。
生物活性

MYCMI-6 (NSC354961) is a potent and selective endogenousMYC:MAXprotein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with aKdof 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 inducesapoptosis[1].

体外研究
(In Vitro)

MYCMI-6 (NSC354961) (6.25 μM; 48 hours) selectively suppresses MYC-driven tumor cell growth with high efficacy[1].
MYCMI-6 significantly inhibits growth of Burkitt’s lymphoma cells (Mutu, Daudi and ST486) - another classical example of a MYC-driven tumor, having translocations ofMYCto one of the immunoglobulin loci - in a dose-dependent manner with an average GI50of 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 IC50for 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 IC50of 3.8 μM. MYCMI-6 efficiently inhibits anchorage-independent growth ofMYCN-amplified neuroblastoma cells with GI50values of<0.4 μM[1].

Cell Viability Assay[1]

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 theMYCN-amplified cell lines significantly stronger than theMYCN-non-amplified cell lines.
体内研究
(In Vivo)

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[1].

Animal Model:6-8 weeks old athymic nude mice (bearing MYCN-amplified SK-N-DZ neuroblastoma cells)[1]
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.
分子量

373.41

性状

Solid

Formula

C20H19N7O

CAS 号

681282-09-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 2.4 mg/mL(6.43 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6780 mL13.3901 mL26.7802 mL
5 mM0.5356 mL2.6780 mL5.3560 mL
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。