KO-947
目录号 : GC33051
An ERK inhibitor
Cas No.:1695533-89-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
KO947 is an ERK inhibitor (IC50 = <50 nM for ERK2).1,2 It is greater than 50-fold selective for ERK over a panel of 450 kinases.1 KO947 reduces phosphorylation of the ERK target p90 ribosomal S6 kinase (RSK) in A375 cancer cells containing constitutively active B-RAFV600E with an IC50 value of less than 250 nM.2 It inhibits proliferation of A375 cells, as well as mutant K-Ras-expressing HCT116 and H358 cancer cell lines (IC50s = 50-250 nM for all).
1.Burrows, F., Kessler, L., Chen, J., et al.Abstract 5168: KO-947, a potent ERK inhibitor with robust preclinical single agent activity in MAPK pathway dysregulated tumorsCancer Res.77(13 Suppl.)5168-5168(2017) 2.Li, L., Wu, T., Feng, J., et al.Inhibitors of ERK and methods of use(2015)
| Cas No. | 1695533-89-1 | SDF | |
| Canonical SMILES | O=C1NC2=CC(NN=C3C4=CC=NC=C4)=C3C=C2CN1CC5=CC=CC=C5 | ||
| 分子式 | C21H17N5O | 分子量 | 355.39 |
| 溶解度 | DMSO : 62.5 mg/mL (175.86 mM) | 储存条件 | 4°C, protect from light |
| 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 | 2.8138 mL | 14.0691 mL | 28.1381 mL |
| 5 mM | 0.5628 mL | 2.8138 mL | 5.6276 mL |
| 10 mM | 0.2814 mL | 1.4069 mL | 2.8138 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。
From Lab Formulation Development to CTM Manufacturing of KO-947 Injectable Drug Products: a Case Study and Lessons Learned
AAPS PharmSciTech 2021 Jun 2;22(5):168.PMID:34080070DOI:10.1208/s12249-021-02059-x.
Formulation development of KO-947-K mesylate injectable drug products was described. Solution formulations were initially attempted, and key parameters such as drug concentration, buffer, pH, complexing agent, and tonicity modifying agent were carefully evaluated in the lab setting, mainly focusing on solubility and chemical stability. A lead solution formulation was advanced to a scaleup campaign. An unexpected stability issue was encountered, and the root cause was attributed to the heterogeneous liquid freezing process of the formulated solution at -20°C, which had not been captured in the lab setting. A lyophilized product was then designed to overcome the issue and supplied to the phase I clinical trial.