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Imatinib Mesylate (STI571). (Synonyms: 甲磺酸伊马替尼 (标准品); STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard))
目录号: PC15924 纯度: ≥98%
CAS No. :220127-57-1
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中文名称
Imatinib Mesylate (STI571).
中文别名
甲磺酸伊马替尼;4-[(4-甲基-1-哌嗪基)甲基]-N-[4-甲基-3-[4-(3-吡啶基)-2-嘧啶基]氨基]苯基]苯甲酰胺甲磺酸盐;4-[(4-甲基-1-哌嗪基)甲基]-N-[4-甲基-3-[4-(3-吡啶基)-2-嘧啶基]氨基]-苯基]苯甲酰胺甲磺酸盐;依马替尼;格列维克;甲磺酸依马替尼;伊马替尼甲磺酸盐;2-(4-甲氧基苯氧基)丙酸;格列卫;甲磺酸阿帕替尼;甲磺酸伊马替尼(A和B);甲磺酸伊马替尼(格列卫);甲硫酸伊马替尼;伊马替尼;左旋舒必利;IMA锡IB甲磺酸盐;甲磺酸伊玛替尼;格列维克原材料;甲磺酸伊马替尼(抗肿瘤)
英文名称
Imatinib Mesylate (STI571)
英文别名
Imatinib Mesylate;4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-benzamide monomethanesulfonate;4-[(4-methylpiperazin-1-yl)methyl]-n-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide methanesulfonate;CGP-57148B;GLEEVEC;GLIVEC;IMATINIB METHANESULFONATE;STI-571;IMATINIB BASE(IMA-3);Imatinib Methanesulfonate, STI-571, CGP-57148B, Glivec;IMATINIB MESYLATE (IMATINIB METHANESULFONATE);alpha-IMATINIB MESYLATE;Imatinib mesylate(TINIBS );Imatinib Mesylate (STI571);4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benzamide methanesulfonic aci...;4-(4-Methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benzamide methanesulfonic acid salt;Gleevec (Imatinib Mesylate);Imatinib;Imatinib (mesylate);Imatinib Mesilate;Imatinib Mesylate (Imatinib Methanesulfonate,Gleevec®,Glivec® );Imatinnib Mesylate;matinib mesylate;Gleevac;Imantinib mesylate;Imatinib mesylate;4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate;4-[(4-Methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide mesylate;CGP 57148;Genfatinib;imatinib monomesylate;CGP 57148B;Imatinib, methanesulfonate salt;8A1O1M485B;STI 571;Imatinib mesylate, 98%;Imatinib mesylate (USAN);Imatinib mes;Imatinib mesylate [USAN];DSSTox_RID_79501;DSSTox_CID_20502;DS
Cas No.
220127-57-1
分子式
C30H35N7O4S
分子量
589.71
包装储存

Sealed and stored at 4℃,, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.

性状

Solid

IC50 & Target[1][2]

IC50: ~100 nM (c-Kit, Bcr-Abl, and PDGFR)

体外研究(In Vitro)

Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM. Imatinib (STI571) mesylate is very effective (体外研究 IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (体外研究 IC50, 410 nM) and PDGFR (体外研究 IC50, 380 nM). Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph) acute lymphoblastic leukemia (ALL).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesylate attenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃,, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 125 mg/mL (211.97 mM; Need ultrasonic)

H2O : ≥ 50 mg/mL (84.79 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6957 mL 8.4787 mL 16.9575 mL
5 mM 0.3391 mL 1.6957 mL 3.3915 mL
10 mM 0.1696 mL 0.8479 mL 1.6957 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 100 mg/mL (169.57 mM); Clear solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.53 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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