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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Protein Tyrosine Kinase/PTK > Imatinib MesylateCAS：220127-57-1
Molecular Formula：C29H31N7O·CH4O3S
Molecular Weight：589.71
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to light yellow Solid
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| CAS | 220127-57-1 |
| Name | Imatinib Mesylate |
| Molecular Formula | C29H31N7O·CH4O3S |
| Molecular Weight | 589.71 |
| Solubility | Soluble in Water ≥50mg/mL;Soluble in DMSO/Ethanol ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to light yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 606-892-3 |
| MDL | MFCD04307699 |
| SMILES | O=S(O)(C)=O.O=C(NC1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4 |
| Target Point | Bcr-Abl;PDGFR;c-Kit |
| Passage | Angiogenesis; Protein Tyrosine Kinase/RTK |
| Background | Imatinib Mesylate is a tyrosine kinase inhibitor that inhibits c-Kit， Bcr-Abl， and PDGFR. |
| Biological Activity | Imatinib Mesylate 是一种酪氨酸激酶抑制剂, 可抑制 c-Kit, Bcr-Abl 和 PDGFR (IC50=100 nM) 。 |
| IC50 | IC50: ~100nM (c-Kit， Bcr-Abl， and PDGFR) [1] |
| In Vitro | 伊马替尼(STI571)甲磺酸盐抑制c-Kit自身磷酸化，MAPK活化和Akt活化而不改变c-kit，MAPK或Akt的总蛋白水平。对这些影响产生50％抑制的浓度约为100 nM [1]。伊马替尼(STI571)甲磺酸盐对引起慢性粒细胞白血病的激酶Bcr-Abl非常有效(体外IC50为25 nM)。伊马替尼还有效抑制Kit(体外IC50，410 nM)和PDGFR(体外IC50，380 nM)[2]。伊马替尼(STI571)甲磺酸盐是v-Abl，c-Kit的多靶点抑制剂，可抑制Bcr / Abl，v-Abl，Tel / Abl，天然PDGFβ受体和c-Kit，但不抑制Src家族激酶，c-Fms，Flt3，EGFR或多种其他酪氨酸激酶。伊马替尼抑制表达Bcr / Abl，Tel / Abl，Tel /PDGFβR和Tel / Arg的Ba / F3细胞的酪氨酸磷酸化和细胞生长，每种情况下IC50约为0.5μM，但对未转化的Ba / F3没有影响。细胞在IL-3或通过Tel / JAK2转化的Ba / F3细胞中生长[3]。甲磺酸伊马替尼选择性地抑制Bcr / Abl，c-Kit和PDGFR激酶的活性。甲磺酸伊马替尼在慢性粒细胞白血病(CML)和费城阳性(Ph +)急性淋巴细胞白血病(ALL)中显示出明显和快速的抗白血病活性[4]。 |
| In Vivo | 用甲磺酸伊马替尼治疗的动物在整个研究中显示平均体重减少。接受化疗和维生素D类似物联合治疗的小鼠体重明显减轻。在实验的第22天，用甲磺酸伊马替尼和PRI-2191联合治疗的小鼠的体重减轻最高(15％)，但在那天之后，小鼠开始恢复[4]。在大鼠缺血/再灌注损伤(IRI)模型中，甲磺酸伊马替尼通过抗渗透和抗炎作用减弱肺损伤。在该模型中也证实了甲磺酸伊马替尼在肺中的传递和功能[5]。 |
| Cell Experiment | 在加入测试化合物之前24小时，将测试的A549细胞以每孔5×103个细胞的密度置于96孔平底板中。将细胞与两种不同浓度(10和100 nM)的PRI-2191孵育96小时，同时与不同浓度的甲磺酸伊马替尼(10，100，1000和10，000 ng / mL)和其他细胞抑制药物(多西紫杉醇(DTX))孵育或Idarubicin(ID)：0.1，1，10，100ng / mL; 顺铂(CIS)：1，10，100，1000ng / mL)。进行磺酰罗丹明B(SRB)测定以评估细胞毒性作用。结果，在Cheburator 0.4，Dmitry Nevozhay软件[4]中为每个单独的实验计算IC50。 |
| Animal Experiment | 使用12-16周龄，体重20-25g的小鼠[4] NOD / SCID雌性小鼠。用A549肿瘤细胞悬浮液(每只小鼠0.2mL Hank培养基中5×10 6个细胞，第0天)将小鼠皮下(sc)接种在腹部右侧，然后随机分成接受维生素D类似物的不同组合的组和化疗。在相应的实验中应用两个实验方案中的一个：1。在接种肿瘤细胞后(当肿瘤变得可触知时)从第7天开始治疗。甲磺酸伊马替尼以75mg / kg /天的剂量腹膜内(ip)给药，每天给药19天(从第7-25天开始)。 PRI-2191以2μg/ kg /天的剂量或通过口服强饲法施用，每周3次(在第7，12，14，16，19，21和23天)。 2.在接种肿瘤细胞后(当肿瘤变得可触知时)从第7天开始治疗。甲磺酸伊马替尼以50mg / kg /天的剂量腹膜内(ip)给药，每天给药13天(从第7-19天开始)。 PRI-2191和PRI-2205分别以1或10μg/ kg /天的剂量皮下施用，每周3次(在第7，10，12，14，17，19，21，24和26天)。在实验结束时，在麻醉下收集血液; 然后，将小鼠处死。大鼠[5]在实验中使用重270至320g的雄性Lewis大鼠。在伊马替尼组(n = 7)腹膜内注射甲磺酸伊马替尼(50mg / kg)，在载体组中给予0.5mL不含伊马替尼的20％DMSO(n = 7)。初步测试25mg / kg的剂量，并且其在肺功能方面产生少许改善而没有统计学意义。根据该结果和过去的报告，采用50mg / kg的剂量和腹膜内给药。将动物进行左胸廓切开术，并用小金属夹闭塞左肺门。在伊马替尼或载体给药后20分钟进行闭塞。夹紧期间，潮气量(TV)和呼吸频率(RR)分别调整为8 mL / kg和80次/ min。缺血90分钟后，取出夹子并保持再灌注120分钟。在再灌注期间，双侧肺部恢复血流和通气。在假手术组(n = 6)中，将动物肝素化，胸腔切开并通气210分钟。 |
| Data Literature Source | [1]. Heinrich MC， et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571， a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1; 96 (3) :925-32. [2]. Guida T， et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1; 13 (11) :3363-9. [3]. Okuda K， et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15; 97 (8) :2440-8 [4]. Maj E， et al. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13; 16 (11) :27191-207. [5]. Tanaka S， et al. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Jul 23. pii: S0003-4975 (16) 30523-9 [6]. Meirson T， et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24; 9 (31) :22158-22183 |
| Unit | Bottle |
| Specification | 100mg 10mM*1mL in DMSO 10mM*1mL in Water 200mg 500mg |
Examples of using this product（for reference only）
In Vivo:
Mice（Six-week-old nude mice; 10 mg/kg IM）:
Murine xenograft modelSix-week-old nude mice were randomly assigned to four groups (n = 6). K562/IM cells(5x105) were stably transfected with sh-circ_0080145 or sh-NC and then injected subcutaneously into mice. After 7d of inoculation, the mice were treated with or without 10 mg/kg IM (Solarbio) every 4d. Tumor length and width were examined every 4d and tumor volume was calculated with the equation: (length · width2 )/2. Twentyseven days later, the mice were euthanized.
Reference：
Che H, Ding H, Jia X. circ_0080145 Enhances Imatinib Resistance of Chronic Myeloid Leukemia by Regulating miR-326/PPFIA1 Axis. Cancer Biother Radiopharm. 2020 Jun 27. doi: 10.1089/cbr.2020.3600. Epub ahead of print. PMID: 32598170.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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Che H, Ding H, Jia X. Cancer Biother Radiopharm. 2020 Jun 27.
Sorry, there is no more information.
circ_0080145 Enhances Imatinib Resistance of Chronic Myeloid Leukemia by Regulating miR-326/PPFIA1 Axis
Click to check >>Author：Che H. Ding H. Jia X
IF：2.6460
Publish_to：Cancer Biother Radiopharm
PMID：32598170
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