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/ Imatinib/伊马替尼

Imatinib/伊马替尼 {[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/伊马替尼 化学结构 CAS号：152459-95-5
Imatinib/伊马替尼 化学结构
CAS号：152459-95-5
Imatinib/伊马替尼 3D分子结构
CAS号：152459-95-5
Imatinib/伊马替尼 化学结构 CAS号：152459-95-5
Imatinib/伊马替尼 3D分子结构 CAS号：152459-95-5
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Imatinib/伊马替尼 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 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 2HCl ++++

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%
(E/Z)-SIS3 free base ✔ 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

 		99%
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 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 ++++

u-Abl1 (T315I), IC50: 5 nM

p-Abl1 (native), IC50: 0.75 nM

 		FLT3,Tie-2 99%+
PP121 ++

Abl, IC50: 18 nM

 		VEGFR,PDGFR 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

 		98%
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/Deubiquitinase 99+%
GNF-5 ++

Bcr-Abl, IC50: 220 nM

 		99%
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。
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

 		97%
Ki8751 ++

c-Kit, IC50: 40 nM

 		99%
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

 		99%
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 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

 		97%
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

 		VEGFR,mTOR 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 99%
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

 		FLT3,c-Kit 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

 		99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit 99%
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit 99%+
Sorafenib ++

mPDGFRβ, IC50: 57 nM

PDGFRβ, 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。

Imatinib/伊马替尼 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/伊马替尼 细胞实验

Cell Line
Concentration Treated Time Description References
GIST-T1 0.05, 0.5 µM 72 h Evaluate the effect of imatinib on proliferation and apoptosis of GIST-T1 cells. Results showed that imatinib treatment increased apoptosis, with nuclear fragmentation increasing from 2.2% to 17.7%. Br J Cancer. 2020 Feb;122(3):372-381.
K562 cells 200 nM 24 and 48 h Combination of imatinib with GSI reduced K562 colony formation and enhanced the inhibition of NOTCH1 signaling J Pathol. 2013 Nov;231(3):378-87.
abl pre-B cells 3 µM 2 days To arrest abl pre-B cells in G0/G1 phase Elife. 2021 Sep 3;10:e68466.
K562 cells 3 μM To evaluate the cytotoxic effect of Imatinib on K562 cells, results showed that erythropoietin (EPO) conferred resistance to Imatinib. Nat Med. 2017 Apr;23(4):472-482.
BaF3-BA cells 3 μM To evaluate the cytotoxic effect of Imatinib on BaF3-BA cells, results showed that the presence of IL-3 conferred resistance to Imatinib. Nat Med. 2017 Apr;23(4):472-482.
BaF3-LTBA cells 3 μM To evaluate the cytotoxic effect of Imatinib on BaF3-LTBA cells, results showed that the presence of IL-3 conferred resistance to Imatinib. Nat Med. 2017 Apr;23(4):472-482.
GIST48 0.5, 1 µM 72 h Evaluate the effect of imatinib on proliferation and apoptosis of GIST48 cells. Results showed that imatinib treatment increased apoptosis, with nuclear fragmentation increasing from 0.1% to 50.1%. Br J Cancer. 2020 Feb;122(3):372-381.
GIST430/654 0.5, 1 µM 72 h Evaluate the effect of imatinib on proliferation and apoptosis of GIST430/654 cells. Results showed that imatinib treatment increased apoptosis, with nuclear fragmentation increasing from 1.6% to 12.3%. Br J Cancer. 2020 Feb;122(3):372-381.
GIST882 0.05, 0.5 µM 72 h Evaluate the effect of imatinib on proliferation and apoptosis of GIST882 cells. Results showed that imatinib treatment increased apoptosis, with nuclear fragmentation increasing from 0.9% to 15.3%. Br J Cancer. 2020 Feb;122(3):372-381.

Imatinib/伊马替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Balb/c nude mice K562 cell xenograft model Intraperitoneal injection 100 mg/kg body weight 10 consecutive days Overexpression of RalA reduced overall survival of recipient mice undergoing IM treatment, indicating that RalA imparts some resistance to IM. Oncotarget. 2016 Apr 12;7(15):20561-73.
Mouse Pten/Braf/Bcat-STA mouse model Oral gavage 200 mg/kg Daily Imatinib significantly slowed the growth of the primary tumor in Pten/Braf/Bcat-STA mice but did not alter the frequency of metastasis. Cancer Cell. 2011 Dec 13;20(6):741-54
Mice Atherosclerosis model Intraperitoneal injection 100 mg/kg Once daily for seven days Imatinib treatment resulted in significant reductions in the percentage of Myh11 -eYFP+ and Myh11 -eYFP+ ACTA2+ cells in the fibrous cap, indicating that non-SMC-derived cells were unable to compensate for the rapid loss of SMC-derived ACTA2+ cells. Nat Metab. 2021 Feb;3(2):166-181
Mice A431, LLC, and T241 tumor models Oral 50 mg/kg Once daily, until primary tumor removal Imatinib significantly inhibited TAM recruitment in A431, LLC, and T241 tumors, indicating that PDGFRs mediate PDGF-BB-induced TAM infiltration. Nat Commun. 2016 May 6;7:11385
Mice AT-GFP mice Intraperitoneal injection 50 mg per mouse Four times a week for 4 weeks Imatinib treatment improved glucose sensitivity and blunted subcutaneous and visceral fat expansion. Additionally, imatinib treatment displaced AT-GFP+APCs from their vascular niche and inhibited white adipocyte differentiation. Nat Commun. 2017 Jun 26;8:15926
Mice BCR-ABL-induced chronic myeloid leukemia model Intraperitoneal injection 75 mg/kg Twice daily for 3 months To evaluate the therapeutic effect of Imatinib on BCR-ABL-induced leukemia in mice, results showed that Imatinib alone could not completely eradicate leukemic cells, but the combination of DFC and BCI completely eradicated leukemic cells. Nat Med. 2017 Apr;23(4):472-482.
Nude mice CML xenograft model Subcutaneous injection 20 mg/kg Once daily for 14 days Evaluate the effect of USP10 inhibition on CML xenograft models Cell Discov. 2019 Apr 30;5:24.

Imatinib/伊马替尼 动物研究

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

Imatinib/伊马替尼 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/伊马替尼 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/伊马替尼 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/伊马替尼 技术信息

CAS号152459-95-5
分子式C29H31N7O
分子量 493.6
SMILES Code O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5CCN(C)CC5)C=C4
MDL No. MFCD05662257
别名 STI571; CGP-57148B
运输蓝冰
InChI Key KTUFNOKKBVMGRW-UHFFFAOYSA-N
Pubchem ID 5291
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

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/伊马替尼 纯度/质量文件 | Imatinib/伊马替尼 亚型比较 | Imatinib/伊马替尼 生物活性 | Imatinib/伊马替尼 动物研究 | Imatinib/伊马替尼 临床数据 | Imatinib/伊马替尼 参考文献 | Imatinib/伊马替尼 实验方案 | Imatinib/伊马替尼 技术信息

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