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/ Imatinib

伊马替尼 /Imatinib {[allProObj[0].p_purity_real_show]}

货号：A150400 同义名： STI571;CGP-57148B

Imatinib (STI571) 是一种口服生物可利用的酪氨酸激酶抑制剂，通过在 ATP 结合位点附近结合，选择性抑制 BCR/ABL、v-Abl、PDGFR 和 c-kit 激酶活性，将其锁定在关闭或自我抑制的构象中，半竞争性抑制酶活性。它还抑制 SARS-CoV 和 MERS-CoV。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Imatinib 化学结构 CAS号：152459-95-5
Imatinib 化学结构
CAS号：152459-95-5
Imatinib 3D分子结构
CAS号：152459-95-5
Imatinib 化学结构 CAS号：152459-95-5
Imatinib 3D分子结构 CAS号：152459-95-5
规格 价格 会员价 库存 数量
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Imatinib 纯度/质量文件 产品仅供科研

货号：A150400 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		98%
Ki8751 ++

c-Kit, IC50: 40 nM

 		98+%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		98%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

 		Src 98%
Dasatinib ++

c-Kit (D816V), IC50: 37 nM

c-Kit (wt), IC50: 79 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%+
LDN-212854 ++++

ALK1, IC50: 2.4 nM

 		++++

ALK2, IC50: 1.3 nM

 		+

ALK3, IC50: 85.8 nM

 		+

ALK4, IC50: 2133 nM

 		+

ALK5, IC50: 9276 nM

 		99%+
ML347 ++

ALK1, IC50: 46 nM

 		++

ALK2, IC50: 32 nM

 		98%
K02288 ++++

ALK1, IC50: 1.8 nM

 		++++

ALK2, IC50: 1.1 nM

 		++

ALK3, IC50: 34.4 nM

 		+++

ALK6, IC50: 6.4 nM

 		99%+
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

 		++++

ALK2, IC50: 0.8 nM

 		+++

ALK3, IC50: 5.3 nM

 		+++

ALK6, IC50: 16.7 nM

 		99%
LDN-214117 ++

ALK2, IC50: 24 nM

 		98%
DMH-1 +

ALK2, IC50: 107.9 nM

 		99%+
SB-505124 +

ALK4, IC50: 129 nM

 		++

ALK5, IC50: 47 nM

 		99%+
Vactosertib +++

ALK4, IC50: 13 nM

 		+++

ALK5, IC50: 11 nM

 		99%+
Alantolactone ✔ 98%
SIS3 ✔ 97%
Pirfenidone ✔ 98%
Hesperetin ✔ 97%
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

 		98%
GW788388 +++

ALK5, IC50: 18 nM

 		98%
LY364947 ++

TGFβRI, IC50: 59 nM

 		+

TGFβRII, IC50: 0.4 μM

 		98%
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

 		98%
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

 		99%+
LY2109761 ++

TβRI, Ki: 38 nM

 		+

TβRII, Ki: 300 nM

 		99%+
Galunisertib ++

TβRI, IC50: 56 nM

 		98%
SB 431542 +

ALK5, IC50: 94 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 PDGFR ↓ PDGFRα ↓ PDGFRβ ↓ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

 		EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

 		98%
Pazopanib ++

PDGFR, IC50: 84 nM

 		99%
Imatinib +

PDGFR, IC50: 100 nM

 		c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

 		c-Kit 99%
Sennoside B ✔ 99%+
PP121 ++++

PDGFR, IC50: 2 nM

 		mTOR,VEGFR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

 		++++

PDGFRβ, Kd: 3.2 nM

 		99%+
Masitinib +

PDGFRα, IC50: 540 nM

 		+

PDGFRβ, IC50: 800 nM

 		99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

 		c-Kit 98+%
Tivozanib ++

PDGFRα, IC50: 40 nM

 		++

PDGFRβ, IC50: 49 nM

 		99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

 		98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

 		99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

 		++++

PDGFRβ, IC50: 1.6 nM

 		98%
CP-673451 +++

PDGFRα, IC50: 10 nM

 		++++

PDGFRβ, IC50: 1 nM

 		99%+
Telatinib +++

PDGFRα, IC50: 15 nM

 		c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

 		++

PDGFRβ, IC50: 65 nM

 		99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

 		99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

 		98%+
Lactate +++

PDGFRβ, IC50: 27 nM

 		c-Kit,FLT3 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

 		99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit 98%
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		c-Kit,FLT3 99%+
Sorafenib ++

PDGFRβ, IC50: 57 nM

mPDGFRβ, IC50: 57 nM

 		99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

 		FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 Abl ↓ Bcr-Abl ↓ 其他靶点 纯度
NVP-BHG 712 +

c-Abl, IC50: 1.667 μM

 		99%+
KW-2449 +++

Abl, IC50: 14 nM

Abl (T315I), IC50: 4 nM

 		FLT3 99%+
Ponatinib ++++

Abl, IC50: 0.37 nM

 		98%
AT9283 99%+
Imatinib Mesylate +

v-Abl, IC50: 600 nM

 		c-Kit,PDGFR 99%
Danusertib ++

Abl, IC50: 25 nM

 		RET 99%+
Rebastinib ++++

p-Abl1 (native), IC50: 0.75 nM

u-Abl1 (T315I), IC50: 5 nM

 		FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

 		PDGFR,VEGFR 99%+
GNF-7 +++

M351T, IC50: 133 nM

E255V, IC50: 122 nM

 		99%+
Olverembatinib dimesylate ++++

Abl, IC50: 0.34 nM

Abl (G250E), IC50: 0.35 nM

 		99%
Dasatinib monohydrate ++++

Abl , IC50: 0.6 nM

 		Src 98%
Dasatinib ++++

Abl, IC50: 0.6 nM

 		Src 98%
Bafetinib +++

Abl, IC50: 5.8 nM

 		98+%
GNF-2 +

Bcr-Abl (SUP-B15 cell line), IC50: 268 nM

Bcr-Abl (K562 cell line), IC50: 273 nM

 		98%+
Degrasyn +

Bcr-Abl, IC50: 1.8 μM

 		DUB 98+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		98%
Radotinib ++

BCR-ABL1, IC50: 34 nM

 		98+%
PD173955 Src 99%+
Nilotinib ++

Bcr-Abl, IC50: <30 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Imatinib 生物活性

靶点

  • PDGFR

    PDGFR, IC50:100 nM
描述 Imatinib is a multiple target inhibitor with IC50 values of 100nM, 100nM, 38nM, 25nM and 25nM for PDGFR, c-kit, v-Abl, c-abl and bcr-abl (measured by in vitro enzyme assays), respectively, usually used for treatment of chronic myelogenous leukemia (CML)[1][2][3]. In cellular study showed that treatment with Imatinib for 90min could selectively inhibited the autophosphorylation of v-AbI at concentration>3μM in PB-3c cI. 15 cells, PDGF-BB-induced autophosphorylation of PDGFR at concentration>0.3μM in BALB/c 313 cells[1], steel factor–dependent phosphorylation of c-kit and steel factor-dependent activation of Akt at concentration>1μM in M-07e cells, as well as autophosphorylation of an activated mutant form of c-kit and c-kit–dependent activation of MAP kinase/AKT at concentration>0.1μM in HMC-1 cells. Consistent with this, Imatinib showed anti- proliferative effect on HMC-1 cells by 90%-95% at concentration ranging in 0.1μM-10μM, which may due to the abrogation by Imatinib of antiapoptotic effect of mutant c-kit activation. [2]. Intraperitoneal injection with Imatinib at dose of 50mg/kg once daily for 30 days suppressed tumor growth in BALB/c AMuLV and BALB/c 3T3 v-sis cells xenograft mice[1].
作用机制 Imatinib can bind with the ATP binding site of BCR/ABL tyrosine kinase, thus keeps BCR/ABL in an inactive form[4].

Imatinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A498 Growth Inhibition Assay IC50=2.57223 μM SANGER
ALL-PO Growth Inhibition Assay IC50=20.8149 μM SANGER
AM-38 Growth Inhibition Assay IC50=88.3953 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=14.3335 μM SANGER

Imatinib 动物研究

Dose Mice: 100 mg/kg[5] (p.o.)
Administration p.o.

Imatinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01400074 Chronic Myeloid Leukemia Phase 3 Unknown June 2014 Korea, Republic of ... 展开 >> Seoul St. Mary's Hospital Recruiting Seoul, Korea, Republic of, 137-701 收起 <<
NCT01083589 Non-small Cell Lung Cancer Phase 2 Completed - United States, Texas ... 展开 >> UT MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00154349 Philadelphia Chromosome Positi... 展开 >>ve Acute Lymphocytic Leukemia 收起 << Phase 2 Completed - -

Imatinib 参考文献

[1]Buchdunger E, Zimmermann J, et al. Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative. Cancer Res. 1996 Jan 1;56(1):100-4.

[2]Heinrich MC, Griffith DJ, 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.

[3]Druker BJ, Tamura S, et al. Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells. Nat Med. 1996 May;2(5):561-6.

[4]Marcucci G, Perrotti D, et al. Understanding the molecular basis of imatinib mesylate therapy in chronic myelogenous leukemia and the related mechanisms of resistance. Commentary re: A. N. Mohamed et al., The effect of imatinib mesylate on patients with Philadelphia chromosome-positive chronic myeloid leukemia with secondary chromosomal aberrations. Clin. Cancer Res., 9: 1333-1337, 2003. Clin Cancer Res. 2003 Apr;9(4):1248-52.

Imatinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.13mL

2.03mL

1.01mL

20.26mL

4.05mL

2.03mL

Imatinib 技术信息

CAS号152459-95-5
分子式C29H31N7O
分子量 493.6
别名 STI571;CGP-57148B
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 12 mg/mL(24.31 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

IP 2% DMSO+2% Tween80+35% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

Tags: Imatinib | 152459-95-5 | STI571 | CGP-57148B | STI 571 | STI-571 | Bcr-Abl Inhibitor | Protein Tyrosine Kinase/RTK | Anti-infection | Autophagy | Bcr-Abl | PDGFR | c-Kit | SARS-CoV | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Imatinib 纯度/质量文件 | Imatinib 亚型比较 | Imatinib 生物活性 | Imatinib 细胞研究 | Imatinib 动物研究 | Imatinib 临床数据 | Imatinib 参考文献 | Imatinib 实验方案 | Imatinib 技术信息

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