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伊马替尼

规格或纯度: ≥99%

CAS编号: 152459-95-5
分子式: C₂₉H₃₁N₇O
分子量: 493.6
MDL号: MFCD05662257
PubChem编号: 5291

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货号 (SKU)	包装规格	是否现货	价格	数量
I124963-1g	1g	现货
I124963-5g	5g	现货
I124963-25g	25g	现货
I124963-100g	100g	现货

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基本描述

别名	伊马替尼 \| N-(4-甲基-3-((4-(吡啶-3-基)嘧啶-2-基)氨基)苯基)-4-((4-甲基哌嗪-1-基)甲基)苯甲酰胺
英文别名	4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide \| CGP-57148 \| HMS3244P10 \| MFCD05662257 \| NCGC00159456-02 \| HY-15463 \| Imatinibum \| NSC743414 \| NSC-743414 \| CHEBI:45783 \| SY028029 \| 1iep \| Glamox (TN)
规格或纯度	≥99%
英文名称	Imatinib (STI571)
生化机理	IC50 Value: 100 nM (PDGFR) ; 100 nM (c-Kit) Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs) and a number of other malignancies. in vitro: In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively . Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR . Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively
应用	An inhibitor of multiple tyrosine kinases
储存温度	-20°C储存,充氩
运输条件	超低温冰袋运输
备注	250mg卖完停产，不再备货
产品介绍	Imatinib(STI571)是多靶点抑制剂，对 v-Abl，c-Kit和PDGFR的IC50分别为0.6 μM，0.1 μM和0.1 μM。An inhibitor of multiple tyrosine kinases Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. An inhibitor of multiple tyrosine kinases

名称和标识符

IUPAC Name	4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
INCHI	InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
InChi Key	KTUFNOKKBVMGRW-UHFFFAOYSA-N
Canonical SMILES	CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
Isomeric SMILES	CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
PubChem CID	5291
分子量	493.6

数据库链接

CAS Registry No.	152459-95-5
DrugBank Ligand	DB00619
Wikipedia	Imatinib
DiscoveRx TREEspot	Imatinib\|
PubChem CID	5291
ChEBI	CHEBI:45783
ChEMBL Ligand	CHEMBL941
RCSB PDB Ligand	STI
PEP	imatinib
Reactome Reaction	R-HSA-9669859, R-HSA-9674397, R-HSA-9669854, R-HSA-9669900, R-HSA-9674430, R-HSA-9674095
Reactome Drug	R-ALL-9659761
DrugCentral Ligand	1423

化学和物理性质

溶解性	DMSO 3 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
密度	1.3
敏感性	对热、空气敏感
折光率	1.67
沸点	715.75° C
熔点	211-213°C

安全和危险性（GHS）

象形图	Health Hazard
信号词	Danger
危险声明	H341: Suspected of causing genetic defects H351: Suspected of causing cancer H360: May damage fertility or the unborn child H361: Suspected of damaging fertility or the unborn child H362: May cause harm to breast-fed children
预防措施声明	P280,P405,P501,P264,P260,P281,P270,P263,P203,P318
Merck Index	4902

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参考文献

1. Takeuchi K, Koike K, Kamijo T, Ishida S, Nakazawa Y, Kurokawa Y, Sakashita K, Kinoshita T, Matsuzawa S, Shiohara M et al.. (2003) STI571 inhibits growth and adhesion of human mast cells in culture.. J Leukoc Biol, 74 (6): (1026-34). [PMID:12960256]
2. Rhee CK, Kim JW, Park CK, Kim JS, Kang JY, Kim SJ, Kim SC, Kwon SS, Kim YK, Park SH et al.. (2011) Effect of imatinib on airway smooth muscle thickening in a murine model of chronic asthma.. Int Arch Allergy Immunol, 155 (3): (243-51). [PMID:21293142]
3. Ustun C, DeRemer DL, Akin C. (2011) Tyrosine kinase inhibitors in the treatment of systemic mastocytosis.. Leuk Res, 35 (9): (1143-52). [PMID:21641642]
4. Coleman CM, Sisk JM, Mingo RM, Nelson EA, White JM, Frieman MB. (2016) Abelson Kinase Inhibitors Are Potent Inhibitors of Severe Acute Respiratory Syndrome Coronavirus and Middle East Respiratory Syndrome Coronavirus Fusion.. J Virol, 90 (19): (8924-33). [PMID:27466418]
5. Sisk JM, Frieman MB, Machamer CE. (2018) Coronavirus S protein-induced fusion is blocked prior to hemifusion by Abl kinase inhibitors.. J Gen Virol, 99 (5): (619-630). [PMID:29557770]

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