Asciminib (ABL001)
(Synonyms: ABL001) 目录号 : GC32703
An allosteric inhibitor of Abl1
Cas No.:1492952-76-7
Sample solution is provided at 25 µL, 10mM.
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Asciminib is an allosteric inhibitor of Abl1 (IC50 = 0.45 nM).1 It is selective for Abl1 over a panel of more than 60 additional kinases (IC50s = >10 μM), as well as ion channels, nuclear receptors, G protein-coupled receptors (GPCRs), and transporters. Asciminib inhibits the proliferation of Luc-Ba/F3 cells transformed with wild-type Bcr-Abl1 or the drug-resistant mutant Bcr-Abl1T315I (GI50s = 1 and 25 nM, respectively), as well as other drug-resistant mutants.2 It reduces tumor growth in a KCL-22 chronic myelogenous leukemia (CML) mouse xenograft model when administered at a dose of 3 mg/kg twice per day and induces tumor regression at doses of greater than or equal to 7.5 mg/kg twice per day.
1.Wylie, A.A., Schoepfer, J., Jahnke, W., et al.The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1Nature543(7647)733-737(2017) 2.Schoepfer, J., Jahnke, W., Berellini, G., et al.Discovery of asciminib (ABL001), an allosteric inhibitor of the tyrosine kinase activity of BCR-ABL1J. Med. Chem.61(18)8120-8135(2018)
Cell experiment: | Ba/F3 cells are treated with a range concentration of asciminib (0-10000 nM) for 48 h. Cell proliferation is measured using the Britelite luciferase detection assay[1]. |
Animal experiment: | Mice: Asciminib efficacy in three patient-derived ALL systemic xenograft models (ALL-7015, AL-7119 and AL-7155) is assessed by FACS monitoring of the percentage of CD45+ cells per live cell in blood samples taken at varying time points after dosing with either 7.5 mg/kg BID (group 2) or 30 mg/kg BID (group 3) asciminib for 3 weeks[1]. |
References: [1]. Wylie AA, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737. | |
| Cas No. | 1492952-76-7 | SDF | |
| 别名 | ABL001 | ||
| Canonical SMILES | O=C(C1=CC(C2=NNC=C2)=C(N3C[C@H](O)CC3)N=C1)NC4=CC=C(OC(F)(Cl)F)C=C4 | ||
| 分子式 | C20H18ClF2N5O3 | 分子量 | 449.84 |
| 溶解度 | DMSO : ≥ 100 mg/mL (222.30 mM) | 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 | 2.223 mL | 11.1151 mL | 22.2301 mL |
| 5 mM | 0.4446 mL | 2.223 mL | 4.446 mL |
| 10 mM | 0.2223 mL | 1.1115 mL | 2.223 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet