GCN2-IN-7
目录号 : GC68284GCN2-IN-7 (compound 39) 是一种具有口服活性和选择性的 general control nonderepressible 2 (GCN2) 抑制剂 (IC50=5 nM)，具有体内的抗肿瘤活性。
Cas No.:2396465-33-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 5 nM (GCN2)[1]
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].
GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation[1].
Cell Proliferation Assay[1]
| Cell Line: | CD8+ T cells from WT and GCN2KO cells |
| Concentration: | 600 nM |
| Incubation Time: | 3 days |
| Result: | Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM. |
GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose[1].
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model[1].
| Animal Model: | Balb/c mice injected with RENCA cells[1] |
| Dosage: | 15 mg/kg |
| Administration: | Oral gavage; 15 mg/kg; BID; 17 days |
| Result: | Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group. |
| Animal Model: | LL2 syngeneic mouse model[1] |
| Dosage: | 50 mg/kg |
| Administration: | Oral gavage; 50 mg/kg; BID; 17 days |
| Result: | Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group. |
[1]. Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20.
| Cas No. | 2396465-33-9 | SDF | Download SDF |
| 分子式 | C22H23BrN8OS | 分子量 | 527.44 |
| 溶解度 | 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 | 1.896 mL | 9.4798 mL | 18.9595 mL |
| 5 mM | 0.3792 mL | 1.896 mL | 3.7919 mL |
| 10 mM | 0.1896 mL | 0.948 mL | 1.896 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。