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: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 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, 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。

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	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。

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

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Imatinib Mesylate 质控信息

Imatinib Mesylate 生物活性

Imatinib Mesylate 细胞研究

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Imatinib Mesylate 参考文献

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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]}

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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

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总药量计算器

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Imatinib Mesylate 纯度/质量文件产品仅供科研