Imatinib Mesylate | STI571 Mesylate;CGP-57148B Mesylate;STI-571;CGP57148B;Imatinib (mesylate) | 伊马替尼甲磺酸盐 | Tyrosine / EGF Receptor Protein Kinase Inhibitor | Bcr-Abl | PDGFR | c-Kit | TGF-beta/Smad

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甲磺酸伊马替尼 /Imatinib Mesylate {[allProObj[0].p_purity_real_show]}

货号：A265691 同义名： 伊马替尼甲磺酸盐 / STI571 Mesylate;CGP-57148B Mesylate

Imatinib Mesylate (STI571 Mesylate) 是一种酪氨酸激酶抑制剂，靶向 c-Kit、Bcr-Abl 和 PDGFR，IC50 为 100 nM。

Imatinib Mesylate 化学结构
CAS号：220127-57-1

Imatinib Mesylate 3D分子结构
CAS号：220127-57-1

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Imatinib Mesylate 纯度/质量文件产品仅供科研

货号：A265691 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
c-Kit 亚型比较
PDGFR 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	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	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl (T315I), IC50: 4 nM Abl, IC50: 14 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		Tie-2,FLT3	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ E255V, IC50: 122 nM M351T, IC50: 133 nM			99%+
Olverembatinib dimesylate	++++ Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 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 (K562 cell line), IC50: 273 nM Bcr-Abl (SUP-B15 cell line), IC50: 268 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。

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 (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 nM	Src	98%
Dasatinib	++ c-Kit (wt), IC50: 79 nM c-Kit (D816V), IC50: 37 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				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			++ 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 Mesylate 生物活性

靶点	PDGFR PDGFR, IC50:100 nM c-Kit c-Kit, IC50:100 nM Abl v-Abl, IC50:600 nM
描述	Imatinib Mesylate is the mesylate form of Imatinib. 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 Mesylate 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
DU145	20 μM	Cell Viability Assay	6-72 h	decreases cell viability	25786656
DU145	20 μM	Apoptosis Assay	48/72 h	induces cell death by apoptosis	25786656
GIST882		Growth Inhibition Assay	96 h	IC50=1.7 μM	24900212
Hep G2		Growth Inhibition Assay		IC50=31 μM	25863232

Imatinib Mesylate 动物研究

Dose	Mice: 50 mg/kg, 150 mg/kg^[5] (i.p.); 100 mg/kg, 200 mg/kg^[6] (p.o.)
Administration	i.p., p.o.

Imatinib Mesylate 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 Mesylate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.48mL

1.70mL

0.85mL

16.96mL

3.39mL

1.70mL

Imatinib Mesylate 技术信息

CAS号	220127-57-1
分子式	C₃₀H₃₅N₇O₄S
分子量	589.708

别名	伊马替尼甲磺酸盐 ;STI571 Mesylate;CGP-57148B Mesylate;STI-571;CGP57148B;Imatinib (mesylate)
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 120 mg/mL(203.49 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

H₂O: 50 mg/mL(84.79 mM)

动物实验配方

PO 0.5% CMC-Na 17 mg/mL suspension

甲磺酸伊马替尼 /Imatinib Mesylate {[allProObj[0].p_purity_real_show]}

Imatinib Mesylate 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Imatinib Mesylate 质控信息

Imatinib Mesylate 生物活性

Imatinib Mesylate 细胞研究

Imatinib Mesylate 动物研究

Imatinib Mesylate 参考文献

Imatinib Mesylate 实验方案

Imatinib Mesylate 技术信息

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PDGFR	PDGFR, IC50:100 nM
c-Kit	c-Kit, IC50:100 nM
Abl	v-Abl, IC50:600 nM

甲磺酸伊马替尼 /Imatinib Mesylate {[allProObj[0].p_purity_real_show]}

Imatinib Mesylate 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Imatinib Mesylate 质控信息

Imatinib Mesylate 生物活性

Imatinib Mesylate 细胞研究

Imatinib Mesylate 动物研究

Imatinib Mesylate 参考文献

Imatinib Mesylate 实验方案

Imatinib Mesylate 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Imatinib Mesylate 纯度/质量文件产品仅供科研