KJ Pyr 9
目录号 : GC14413
An inhibitor of c-Myc and v-Myc interaction with Max
Cas No.:581073-80-5
Sample solution is provided at 25 µL, 10mM.
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Target: MYC
Kd value: 6.5 ± 1.0 nM
KJ Pyr 9 is a novel small molecule inhibitor of MYC, with the Kd value of 6.5 ± 1.0 nM. Besides, KJ Pyr 9 also suppresses the formation of MYC-MAX and oncogenic transformation induced by MYC in cell culture [1].
In Vitro: In chicken embryo fibroblasts, KJ Pyr 9 was found to have the ability to interfere with the oncogenic activity of MYC, with the best aqueous solubility. Besides, in human B-cell line P493-6, 20 μM KJ Pyr 9 could significantly inhibit cell proliferation, and KJ Pyr 9 could also inhibit the proliferation of NCI-H460, MDA-MB-231, and SUM-159PT cell lines, with the IC50 values between 5-10 μM. Furthermore, treatment of P493-6 cells with KJ Pyr 9 could significantly suppress the transcription ability of MYC [1].
In Vivo: KJ Pyr 9 was found to have no acute toxicity in mouse and rat at a dose of 10 mg/kg, with an impressive ability to cross the blood-brain barrier. Besides, in a MDA-MB-231 cells xenograft tumor nude mice model, intraperitoneal injection with 10 mg/kg KJ Pyr 9 for 31 days could significantly inhibit tumor growth, while having no effect on the body weight [1].
Clinical trial: No data available recently.
Reference:
[1] Hart J R, Garner A L, Yu J, et al. Inhibitor of MYC identified in a Kröhnke pyridine library[J]. Proceedings of the National Academy of Sciences, 2014, 111(34): 12556-12561.
Cell experiment: | Assays used staining with the redox dye resazurin to measure cell viability. Cells are seeded at 103 per 100 μL well in 96-well plates and grown in the presence of 2.5% FBS. MDA-MB-231 cells are cultured in DMEM; SUM-159PT cells are cultured in HAM’s F12; and NCI-H460 cells are cultured in RPMI-1640. MDA-MB-231 cells are exposed to KJ Pyr 9 (KJ-Pyr-9) for 216 h with fresh compound-containing medium supplied at 120 and 192 h; SUM-159PT cells are exposed to the compound for 120 h and fresh medium with the appropriate compound concentrations is supplied at 48 h; and NCI-H460 cells are grown with compound for 72 h. Triplicate cultures of P493-6 cells are grown in six-well plates from a starting density of 1×105 cells per mL in 4 mL culture medium per well. Compounds are added immediately following cell seeding. Following compound addition, cells are distributed by vortexing the plate at 400 rpm for 10 s. One hundred-microliter samples are taken after vortexing and counted using a Beckman Coulter Z1 counter at 0, 12, 24, 36, 48, 60, 72, and 96 h of incubation[1]. |
Animal experiment: | Mice[1] Ten 8-wk-old female nude mice (HSD:athymic nude-Foxn1nu) are injected with 5×106 MDA-MB-231 cells s.c. into the left and right flanks. Cells are suspended in high-concentration Matrigel before injection. Xenograft tumors are allowed to grow until the average volume of the tumors reached 100 mm3, as measured by external calipers. At this point, the mice are divided into two groups. One receive 10 mg/kg KJ Pyr 9 and the other receive vehicle only, dosed daily by i.p. injection. Tumor volume and mouse weight are measured daily. Vehicle used in all cases is 10:10:80 Tween 80:DMSO:5% dextrose in water. The mice are treated for a period of 31 d. At the end of the experiment, the mice are euthanized and tumors are excised. Tumors are weighed. Samples of each tumor are fixed in formalin for histology and frozen for Western blotting. |
References: [1]. Hart JR, et al. Inhibitor of MYC identified in a Kr hnke pyridine library. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12556-61. | |
| Cas No. | 581073-80-5 | SDF | |
| 化学名 | 4-[2-(2-furanyl)-6-(4-nitrophenyl)-4-pyridinyl]-benzamide | ||
| Canonical SMILES | NC(C(C=C1)=CC=C1C2=CC(C3=CC=CO3)=NC(C4=CC=C([N+]([O-])=O)C=C4)=C2)=O | ||
| 分子式 | C22H15N3O4 | 分子量 | 385.4 |
| 溶解度 | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5947 mL | 12.9735 mL | 25.9471 mL |
| 5 mM | 0.5189 mL | 2.5947 mL | 5.1894 mL |
| 10 mM | 0.2595 mL | 1.2974 mL | 2.5947 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet