Imatinib

SKU: orb1300957

描述

Imatinib (STI571) is an orally active small molecule that potently and selectively inhibits the tyrosine kinases BCR-ABL, PDGFR, and c-Kit. It is widely used in research for chronic myeloid leukemia (CML), gastrointestinal stromal tumors (GIST), and in vitro studies of oncogenic signaling pathways.

研究领域

Cardiovascular Research, Cell Biology, Infectious Disease & Virology, Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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关键属性

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CAS 号	152459-95-5
MW	493.6027
纯度	>99.99% (May vary between batches)
分子式	C₂₉H₃₁N₇O
SMILES	CN1CCN(CC2=CC=C(C=C2)C(=O)NC2=CC(NC3=NC=CC(=N3)C3=CN=CC=C3)=C(C)C=C2)CC1
靶点	Bcr-Abl,Autophagy,SARS-CoV,c-Kit,PDGFR
溶解性	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5.06 mM);DMSO:25 mg/mL (50.65 mM)

生物活性

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靶点 IC50	BV-173 cells:20 μM\|MG-63 cells:20 μM\|ASPC1 cells:44 μM\|PDGFR:100 nM (cell free)\|POS-1 cells:15 μM\|A10 cells:162 nM\|c-Kit:100 nM (cell free)\|HOS cells:11 μM\|OSRGA cells:9 μM\|MOS-J cells:23 μM\|A2780 cells:48 μM\|A431 cells:31 μM\|BaF3 cells:> 1 μM\|BaF3 cells:> 10 μM\|A549 cells:> 25 μM
体内	METHODS: To investigate antitumor activity, Imatinib (25-100 mg/kg) was administered orally to mice bearing undifferentiated POS-1 or mixed osteoblast/osteolytic MOS-J osteosarcoma tumors once daily for 21 or 43 days. RESULTS: Imatinib inhibited osteosarcoma progression in vivo. METHODS: To study the effects on multiple sclerosis (MS), Imatinib (60 mg/kg) was administered orally six times per week for two weeks to an EAE C57BL/6 mouse model. RESULTS: Imatinib had beneficial effects on EAE by reducing disease severity and delaying onset.Imatinib and its potential therapeutic effects and immunomodulatory properties may be considered for the treatment of multiple sclerosis.
体外	METHODS: Human, mouse and rat osteosarcoma cells were treated with Imatinib (1-40 μM) for 72 h, and cell viability was measured using XTT assay. RESULTS: Imatinib reduced the number of live osteosarcoma cells in a dose-dependent manner, with 72 h IC50s of 20 μM (MG-63), 11 μM (HOS), 23 μM (MOS-J), 15 μM (POS-1), and 9 μM (OSRGA). METHODS: Human gastric cancer cells AGS, MKN45 and SNU638 were treated with Imatinib (30-100 μM) for 48 h. Apoptosis was detected using Flow Cytometry. RESULTS: The percentage of Annexin V/PI-positive cells was significantly increased, indicating that Imatinib treatment increased early apoptosis of tumor cells.
细胞研究	M-07e cells were grown in serum-free RPMI 1640 at 37°C for approximately 18 hours before they were incubated for 90 minutes in the presence of various concentrations of STI 571. The cells were then pelleted and resuspended in 1 mL RPMI 1640. STI 571 was added to each tube to achieve the same concentration used during the 90 minutes of preincubation. The cells were then incubated with inhibitor and growth factor (SLF or GM-CSF) for 15 minutes at 37°C. Subsequently, the cell pellets were lysed with 100 to 250 μL of protein lysis buffer (50 mmol/L Tris, 150 mmol/L sodium chloride, 1% NP-40, and 0.25% deoxycholate, with addition of the inhibitors aprotinin, leupeptin, pepstatin, phenylmethyl sulfonyl fluoride, and sodium orthovanadate). Western immunoblot analysis was performed as previously described.41Experiments with HMC-1 cells were performed in the same way except that neither SLF nor GM-CSF was added .
动物研究	Swiss mice (nu/nu, female), weighing 30 g, 6 – 8 weeks old, were bred in the animal facilities, maintained under specific pathogen-free conditions with artificial lighting (12 hr light/12 hr dark cycle) and fed a regular diet and water ad libitum. For therapeutic trials, the tumor-bearing mice were randomly divided into equivalent groups of 5 to 12 animals and mice were treated as soon as the xenografted tumors reached a diameter of 5 mm (or a tumor volume of approximately 60 mm^3). Four different human tumors were used: the SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers. STI571 was administered at a total dosage of 70 or 100 mg/kg per day in 1 or 2 intraperitoneal injections, with or without etoposide plus ifosfamide or topotecan. STI571 was diluted in 150 l of H2O and administered on different days, as indicated. Etoposide and ifosfamide were diluted in 200 l of 0.9% sodium chloride, and topotecan was diluted in 150 l of 0.9% sodium chloride. The control group received injections according to the same schedule as experimentally treated mice. All mice were weighed once weekly. Tumor growth was monitored by measuring 2 perpendicular diameters with calipers. Tumor volume (V) and the relative tumor volume (RTV) were calculated as:. V = a^2 × b/2,. where a is the width (large diameter) and b the length (small. diameter) of the tumor in millimeters, and. RTV = Vx/Vi,. where Vx is the mean tumor volume in cubic millimeters at any given time and Vi is the mean initial tumor volume in cubic millimeters at the start of treatment. Mice were ethically sacrificed when the tumor volume reached 2,500 mm^3 .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Bcr-Abl, BcrAbl, Autophagy, cKit, c-Kit, CD117, CGP057148B, CGP-57148B, Inhibitor, Imatinib, inhibit, Platelet-derived growth factor receptor, PDGFR, ST1571, ST-1571, ST 1571, SCFR, SARSCoV, SARS coronavirus, SARS-CoV, STI 571, STI571, STI-571, v-Abl

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Unconjugated
可选规格： 200 μl, 20 μl
Imatinib impurity 12 [orb3181562]
CAS 号：
1821122-73-9
MW:
888.07
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C₅₃H₅₁N₁₂O₂
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MW:
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C₄₇H₄₆N₁₂O₃
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MW:
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C₂₁H₂₈FN₇O₂
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质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

5291 ↗

关键属性

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暂无计算属性。

实验方案信息

PubMed:

应用：	FC, WB
反应性：	Human
种属/宿主：	Rabbit
克隆性：	Monoclonal
偶联：	Unconjugated

CAS 号：	1821122-73-9
MW:	888.07
分子式：	C₅₃H₅₁N₁₂O₂

CAS 号：	571186-93-1
MW:	525.61
分子式：	C₂₉H₃₁N₇O₃

CAS 号：	1987905-93-0
MW:	826.97
分子式：	C₄₇H₄₆N₁₂O₃

CAS 号：	2999638-62-7
MW:	429.49
分子式：	C₂₁H₂₈FN₇O₂

Imatinib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Phospho-Lck (Tyr505) rabbit mAb Antibody [orb1946120]

Imatinib impurity 12 [orb3181562]

Imatinib impurity 21 [orb3181484]

Imatinib impurity 2 [orb3181465]

BLU-654 [orb3210817]

质量保证

化合物标识

关键属性

实验方案信息

可选规格