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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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 (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	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		PDGFR,c-Kit	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	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。

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 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。

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].

Cell Line GIST48 GIST430/654 GIST882 GIST-T1 LAMAs cells KCL22s cells K562 cells KBM5-T315I cells KBM5 cells K562 cells BaF3-BA cells BaF3-LTBA cells abl pre-B cells human microvascular endothelial cell line HMEC-1 human coronary arterial endothelial cells (HCAEC) human umbilical vein endothelial cells (HUVEC) Mouse bone marrow cells Human peripheral blood mononuclear cells Vero E6 cells Human umbilical vein endothelial cells (HUVECs)	Concentration	Treated Time	Description	References
GIST48	0.5, 1 µM	72 h	Evaluate the effect of imatinib on apoptosis in GIST48 cells, results showed that imatinib treatment led to 39.5% apoptosis.	Br J Cancer. 2020 Feb;122(3):372-381.
GIST430/654	0.5, 1 µM	72 h	Evaluate the effect of imatinib on apoptosis in GIST430/654 cells, results showed that imatinib treatment led to 31% apoptosis.	Br J Cancer. 2020 Feb;122(3):372-381.
GIST882	0.05, 0.5 µM	72 h	Evaluate the effect of imatinib on apoptosis in GIST882 cells, results showed that imatinib treatment led to 14.9% apoptosis.	Br J Cancer. 2020 Feb;122(3):372-381.
GIST-T1	0.05, 0.5 µM	72 h	Evaluate the effect of imatinib on apoptosis in GIST-T1 cells, results showed that imatinib treatment led to 14.3% apoptosis.	Br J Cancer. 2020 Feb;122(3):372-381.
LAMAs cells	200 nM	24 and 48 h	To investigate the effect of imatinib in combination with GSI on LAMAs cells, results showed that the combination treatment significantly reduced NOTCH1 signaling.	J Pathol. 2013 Nov;231(3):378-87.
KCL22s cells	200 nM	24 and 48 h	To investigate the effect of imatinib in combination with GSI on KCL22s cells, results showed that the combination treatment significantly reduced NOTCH1 signaling.	J Pathol. 2013 Nov;231(3):378-87.
K562 cells	200 nM	24 and 48 h	To investigate the effect of imatinib in combination with GSI on K562 cells, results showed that the combination treatment significantly reduced NOTCH1 signaling.	J Pathol. 2013 Nov;231(3):378-87.
KBM5-T315I cells	1 μM	24 h	To evaluate the inhibitory effect of imatinib on Bcr-Abl kinase activity in KBM5-T315I cells, results showed that imatinib had a weaker inhibitory effect on Bcr-Abl kinase activity with T315I mutation	Cell Discov. 2019 Apr 30;5:24.
KBM5 cells	1 μM	24 h	To evaluate the inhibitory effect of imatinib on Bcr-Abl kinase activity in KBM5 cells, results showed that imatinib significantly reduced the phosphorylation level of Bcr-Abl and SKP2 protein level	Cell Discov. 2019 Apr 30;5:24.
K562 cells	3 μM	6 h	Evaluate the inhibitory effect of imatinib on K562 cells, showing that erythropoietin can confer resistance to imatinib.	Nat Med. 2017 Apr;23(4):472-482.
BaF3-BA cells	3 μM	60 h	Evaluate the inhibitory effect of imatinib on BCR-ABL-expressing cells, showing that IL-3 can confer resistance to imatinib.	Nat Med. 2017 Apr;23(4):472-482.
BaF3-LTBA cells	3 μM	60 h	Evaluate the inhibitory effect of imatinib on BCR-ABL-expressing cells, showing that IL-3 can confer resistance to imatinib.	Nat Med. 2017 Apr;23(4):472-482.
abl pre-B cells	3 μM	2 days	To arrest abl pre-B cells in G0/G1 phase for studying DNA double-strand break repair mechanisms	Elife. 2021 Sep 3;10:e68466.
human microvascular endothelial cell line HMEC-1	0.01-20 µM	48 h	To evaluate the effects of Imatinib on endothelial cell growth and function. Results showed that Imatinib had no significant effects on endothelial cell proliferation, migration, or tube formation.	Leukemia. 2017 Nov;31(11):2388-2397.
human coronary arterial endothelial cells (HCAEC)	0.01-20 µM	48 h	To evaluate the effects of Imatinib on endothelial cell growth and function. Results showed that Imatinib had no significant effects on endothelial cell proliferation, migration, or tube formation.	Leukemia. 2017 Nov;31(11):2388-2397.
human umbilical vein endothelial cells (HUVEC)	0.01-20 µM	48 h	To evaluate the effects of Imatinib on endothelial cell growth and function. Results showed that Imatinib had no significant effects on endothelial cell proliferation, migration, or tube formation.	Leukemia. 2017 Nov;31(11):2388-2397.
Mouse bone marrow cells	0-10 μM	48 h	To investigate the effects of imatinib and GW2580 on the differentiation of monocytes into macrophages. Results showed that GW2580 significantly inhibited macrophage formation at lower concentrations.	Arthritis Res Ther. 2010;12(1):R32.
Human peripheral blood mononuclear cells	0-10 μM	48 h	To assess the inhibitory effects of imatinib and GW2580 on c-Fms activity. Results showed that GW2580 significantly inhibited c-Fms activity at lower concentrations.	Arthritis Res Ther. 2010;12(1):R32.
Vero E6 cells	25 μM	6 h	To evaluate the effect of imatinib on SARS-CoV-2 infection, results showed that imatinib dramatically reduced the viral RNA in the cell culture medium by up to 89.1%–99.9%.	Cell Metab. 2022 Mar 1;34(3):424-440.e7.
Human umbilical vein endothelial cells (HUVECs)	25 μM	16 h	To evaluate the effect of imatinib on ACE2 enzymatic activity, results showed that imatinib significantly elevated the enzymatic activity of ACE2.	Cell Metab. 2022 Mar 1;34(3):424-440.e7.

Species Mice Mice Mouse Mice Mice ApoE-/- mice DBA/1 mice Balb/c mice Mice	Animal Model Apoe−/− mice A431, LLC, and T241 tumor models Pten/Braf/Bcat-STA melanoma model AT-GFP mice BCR-ABL-induced chronic myeloid leukemia model Atherosclerosis model Collagen-induced arthritis (CIA) Chronic myeloid leukemia model High-fat-diet-induced insulin-resistant mice	Administration	Dosage	Frequency	Description	References
Mice	Apoe−/− mice	Intraperitoneal injection	100mg/kg/day	Once daily for 7 days	To test the effect of Imatinib on atherosclerotic plaque stability, results showed that Imatinib treatment led to a significant reduction in SMC-derived ACTA2+ cells in the fibrous cap and decreased plaque stability.	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	Nat Commun. 2016 May 6;7:11385
Mouse	Pten/Braf/Bcat-STA melanoma model	Oral gavage	200 mg/kg	Daily administration	Inhibition of Kit receptor signaling significantly slowed growth of the primary tumor, but did not alter the frequency of metastasis.	Cancer Cell. 2011 Dec 13;20(6):741-54
Mice	AT-GFP mice	Intraperitoneal injection	50 mg/mouse	Four times a week for 4 weeks	To evaluate the effect of Imatinib on adipose tissue vascular niche, results showed that imatinib treatment improved glucose sensitivity but blunted subcutaneous and visceral fat expansion and altered APC niche interaction.	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	Evaluate the therapeutic effect of imatinib alone or in combination with DFC and BCI on leukemic mice, showing that combination therapy can eradicate leukemic cells.	Nat Med. 2017 Apr;23(4):472-482.
ApoE-/- mice	Atherosclerosis model	Orally	50 mg/kg	Twice daily for 8 weeks	To evaluate the effects of Imatinib on atherosclerosis. Results showed that Imatinib did not significantly promote atherosclerosis.	Leukemia. 2017 Nov;31(11):2388-2397.
DBA/1 mice	Collagen-induced arthritis (CIA)	Oral	80 mg/kg	Twice daily, for the duration of the experiment	To evaluate the therapeutic efficacy of imatinib in CIA. Results showed that imatinib significantly reduced arthritis severity and histopathologic scores.	Arthritis Res Ther. 2010;12(1):R32.
Balb/c mice	Chronic myeloid leukemia model	Oral gavage	50 mg/kg/day	Once daily for 2 weeks	To evaluate the therapeutic effect of imatinib on the chronic myeloid leukemia model. Results showed that imatinib prolonged the survival of Ba-F3p210 cell-transplanted mice but had no effect on Ba-F3T315I cell-transplanted mice.	Cancer Sci. 2023 Jan;114(1):247-258
Mice	High-fat-diet-induced insulin-resistant mice	Gavage	250 mg/kg	Once daily for 4 weeks	To evaluate the effect of imatinib on metabolic disorders in SARS-CoV-2-infected mice, results showed that imatinib significantly improved insulin resistance and dyslipidemia.	Cell Metab. 2022 Mar 1;34(3):424-440.e7.

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.

CAS号	220127-57-1
分子式	C₃₀H₃₅N₇O₄S
分子量	589.71
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.CS(=O)(O)=O
MDL No.	MFCD04307699

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别名	伊马替尼甲磺酸盐 ;STI571 Mesylate; CGP-57148B Mesylate; STI-571; CGP57148B
运输	蓝冰
InChI Key	YLMAHDNUQAMNNX-UHFFFAOYSA-N
Pubchem ID	123596

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

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
K562		Growth Inhibition Assay		IC50=0.5 μM	24939418
K562		Growth Inhibition Assay		EC50=0.09 μM	16678414
K562		Cytotoxicity Assay	24 h	IC50=0.21 μM	22000207
K-562		Growth Inhibition Assay		IC50=1 μM	25239662
K562r		Growth Inhibition Assay		IC50=10 μM	24939418
MCF-7	10 μM	Growth Inhibition Assay	48 h	blocks cell proliferation increase induced by BJ3Z	25274034
MCF-7		Cytotoxicity Assay	24 h	IC50=0.83 μM	22000207
MDA-MB-23		Cytotoxicity Assay	24 h	IC50=1.8 μM	22000207
PC3	20 μM	Cell Viability Assay	6-72 h	increases cell viability	25786656
PC3	20 μM	Apoptosis Assay	48/72 h	increases cell survival	25786656
T47D		Growth Inhibition Assay		IC50=50 μM	25863232

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