RIPK3-IN-1
目录号 : GC62455
RIPK3-IN-1 是 II 型 RIPK3 DFG-out 位点抑制剂，IC50 为 9.1 nM。RIPK3-IN-1 抑制 RIPK1 和 RIPK2，IC50 为 5.5 和 >10 μM。RIPK3-IN-1 还是 c-Met 激酶抑制剂，IC50 为 1.1 μM。
Cas No.:2361139-70-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM[1].
RIPK3-IN-1 (Compound 18) also inhibits ABL, BRAF/V599E, MAP4K3, and SRC with IC50s of 0.37, 0.15, 0.012, and 0.075 μM, respectively[1].Necroptosis is a programmed form of cell death and has been associated with a variety of diseases, including ischemia reperfusion injury, neurodegenerative disorders, pancreatic cancer, and autoimmune diseases such as inflammatory bowel disease (IBD). Upon stimulation of death receptors (such as the family of TNF receptors), signaling can initiate a necroptotic cell death process. This involves formation of a necrosome, which includes receptor interacting protein kinases 1 and 3 (RIPK1, RIPK3) in a cytosolic complex[1].
[1]. Amy C Hart, et al. Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage. ACS Med Chem Lett. 2019 May 6;11(3):266-271.
| Cas No. | 2361139-70-8 | SDF | |
| 分子式 | C29H25FN4O4 | 分子量 | 512.53 |
| 溶解度 | DMSO : 5 mg/mL (9.76 mM; ultrasonic and warming and heat to 80°C) | 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 | 1.9511 mL | 9.7555 mL | 19.5111 mL |
| 5 mM | 0.3902 mL | 1.9511 mL | 3.9022 mL |
| 10 mM | 0.1951 mL | 0.9756 mL | 1.9511 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。