Imatinib-d3
(Synonyms: STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride) 目录号 : GC47452An internal standard for the quantification of imatinib
Cas No.:1134803-18-1
Sample solution is provided at 25 µL, 10mM.
Imatinib-d3 is intended for use as an internal standard for the quantification of imatinib by GC- or LC-MS. Imatinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit.1 It inhibits ligand-stimulated autophosphorylation of PDGFR and c-Kit (IC50s = ~0.3 and ~0.1 μM, respectively).1,2 Imatinib inhibits the proliferation of Bcr-Abl-dependent R10(-) cells (IC50s = ~35-40 nM) and HMC-1 cells expressing constitutively active c-Kit in a concentration-dependent manner.1,3 It prolongs survival in a mouse model of chronic myeloid leukemia when administered at a dose of 100 mg/kg twice per day.4 Imatinib (25 and 50 µM) also inhibits the replication of Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in Vero E6 cells.5 It reduces viral titers in Vero cells infected with infectious bronchitis virus (IBV), a coronavirus, when used at a concentration of 10 µM via inhibition of IBV surface glycoprotein protein-induced syncytia formation and virus-cell fusion.6 Formulations containing imatinib have been used in the treatment of various cancers.
1.Heinrich, M.C., Griffith, D.J., Druker, B.J., et al.Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitorBlood96(3)925-932(2000) 2.Buchdunger, E., Zimmermann, J., Mett, H., et al.Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivativeCancer Res.56(1)100-104(1996) 3.Wisniewski, D., Lambek, C.L., Liu, C., et al.Characterization of potent inhibitors of the Bcr-Abl and the c-kit receptor tyrosine kinasesCancer Res.62(15)4244-4255(2002) 4.Wolff, N.C., Veach, D.R., Tong, W.P., et al.PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemiaBlood105(10)3995-4003(2005) 5.Coleman, C.M., Sisk, J.M., Mingo, R.M., et al.Abelson kinase inhibitors are potent inhibitors of severe acute respiratory syndrome coronavirus and Middle East respiratory syndrome coronavirus fusionJ. Virol.90(19)8924-8933(2016) 6.Sisk, J.M., Frieman, M.B., and Machamer, C.E.Coronavirus S protein-induced fusion is blocked prior to hemifusion by Able kinase inhibitorsJ. Gen. Virol.99(5)619-630(2018)
Cas No. | 1134803-18-1 | SDF | |
别名 | STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride | ||
Canonical SMILES | O=C(NC1=CC=C(C)C(NC2=NC(C3=CC=CN=C3)=CC=N2)=C1)C(C=C4)=CC=C4CN5CCN(C([2H])([2H])[2H])CC5 | ||
分子式 | C29H28D3N7O | 分子量 | 496.6 |
溶解度 | DMSO: slightly soluble,Methanol: slightly soluble | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0137 mL | 10.0685 mL | 20.1369 mL |
5 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
10 mM | 0.2014 mL | 1.0068 mL | 2.0137 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet