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。
| 生物活性 | MYCi361 (NUCC-0196361) is aMYCinhibitor with the Kdof 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 IC50values[1].
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. |
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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].
| 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.. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(168.11 mM;Need ultrasonic) 配制储备液 | 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℃, 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。 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本网站选购。 |
