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MYCi361

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Chemical Structure| 2289690-31-7 同义名 : NUCC-0196361
CAS号 : 2289690-31-7
货号 : A1251864
分子式 : C26H16ClF9N2O2
纯度 : 99%+
分子量 : 594.856
MDL号 : MFCD32263412
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(176.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MYC proteins, including MYC, MYCL, and MYCN, play critical roles in tumorigenesis and therapeutic resistance. MYCi361 is an inhibitor of MYC that binds to intracellular MYC with a KD of 3.2 μM. Treatment of PC3 cells with MYCi361 (4–10 μM; 0.5 hr) led to significant thermal destabilization of MYC protein. Treatment of PC3 cells with MYCi361 (6 μM; 1 hr) led to disruption of the MYC/MAX interaction. MYCi361 (6 μM) decreased MYC protein stability by modulating MYC-Threonine 58 phosphorylation in PC3 cells. MYCi361 (6 μM; 24 h) also potently suppressed the expression of MYC target genes CDC25A and MYB in MYCT58A-expressing cells. MYCi361 inhibited the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC50 values. MYCi361 treatment of FVB mice bearing established MycCaP tumor allografts at 100 mg/kg/day induced tumor regression[2].
作用机制 MYCi361 binds to amino acids 366–378 of the MYC protein[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.68mL

0.34mL

0.17mL

8.41mL

1.68mL

0.84mL

16.81mL

3.36mL

1.68mL
参考文献

[1]Han H, Jain AD, Truica MI, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019;36(5):483-497.e15. doi:10.1016/j.ccell.2019.10.001

[2]Han H, et al. Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy. Cancer Cell. 2019 Nov 11;36(5):483-497.e15