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Imatinib-d3 Sale

(Synonyms: STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride) 目录号 : GC47452

An internal standard for the quantification of imatinib

Imatinib-d3 Chemical Structure

Cas No.:1134803-18-1

规格 价格 库存 购买数量
500 μg
¥1,352.00
现货
1 mg
¥2,433.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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)

Chemical Properties

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
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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。
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。

溶解性数据

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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
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