MYCi361(Synonyms: NUCC-0196361)

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MYCi361 (Synonyms: NUCC-0196361) 纯度: 99.42%

MYCi361 (NUCC-0196361) 是一种 MYC 抑制剂，其与 MYC 结合的 Kd 为 3.2 μM。MYCi361 (NUCC-0196361) 抑制肿瘤生长并增强 anti-PD1 免疫疗法。

MYCi361(Synonyms: NUCC-0196361)

MYCi361 Chemical Structure

CAS No. : 2289690-31-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4580 In-stock
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
25 mg ￥9900 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

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生物活性

MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy[1].

体外研究
(In Vitro)

MYCi361 inhibits 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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: The prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2).
Concentration: 1.4-5.0 μM
Incubation Time: 5 days
Result: IC50s of 2.9, 1.4, 1.6, 2.6, 5.0, 2.1, and 4.9 μM for prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2), respectively.

体内研究
(In Vivo)

MYCi361 inhibits MYC-dependent tumor growth in vivo. MYCi361 treatment (100 mg/kg/day for 2 days; then 70 mg/kg/day for 9 days) induces tumor regression in FVB or NSG male mice[1].
MYCi361 has moderate terminal elimination half-life of 44 and 20 h for intraperitoneal (i.p.) or oral (p.o.) dosing in mice, respectively[1].
MYCi361 suppresses tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. However, MYCi361 demonstrates a narrow therapeutic index. An improved analog, MYCi975 shows better tolerability[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: FVB or NSG male mice of 6-8 weeks of age and 25 g bearing established MycCaP tumors[1]
Dosage: 50 mg/kg and 70 mg/kg
Administration: Treatment i.p. initially at 50 mg/kg twice daily for 2 days, then 70 mg/kg/day for 9 days
Result: Induced tumor regression.
Animal Model: C57BL/6 mice[1]
Dosage: 50 mg/kg (Pharmacokinetic analysis)
Administration: Treated p.o. or i.p.; 24 hours
Result: Intraperitoneal (i.p.) or oral (p.o.) dosing in mice indicated plasma half-lives of 44 and 20 h, respectively, with maximum plasma concentrations (Cmax) of 27,200 ng/mL (46 μM) i.p. and 13,867 ng/mL (23 μM) p.o..

分子量

594.86

Formula

C26H16ClF9N2O2
CAS 号

2289690-31-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 110 mg/mL (184.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6811 mL 8.4053 mL 16.8107 mL
5 mM 0.3362 mL 1.6811 mL 3.3621 mL
10 mM 0.1681 mL 0.8405 mL 1.6811 mL

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.50 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

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

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