イマチニブメシル酸塩 (Synonyms: Imatinib (Mesylate); STI571 (Mesylate); CGP-57148B (Mesylate))

Name: Imatinib Mesylate
Brand: MedChemExpress
SKU: HY-50946
Rating: 5.0 (120 reviews)

製品番号: HY-50946 純度: 99.93%: Data Sheet SDS COA 取扱説明書
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Technical Support

Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

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CAS 番号 : 220127-57-1

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 72	在庫あり	Estimated Time of Arrival: December 31
Solid
200 mg	$66	在庫あり	Estimated Time of Arrival: December 31
500 mg	$99	在庫あり	Estimated Time of Arrival: December 31
1 g	$145	在庫あり	Estimated Time of Arrival: December 31
5 g	$257	在庫あり	Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 120 publication(s) in Google Scholar

Other Forms of Imatinib Mesylate:

Imatinib-d₈ mesylate 在庫あり
N-Desmethyl imatinib 在庫あり
Imatinib 在庫あり
Imatinib Mesylate (Standard) 在庫あり

顧客検証

Cell Proliferation/Viability Assay

IHC

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]; Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in PC-9 GR NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]; Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jun 1;12(6):e0178619. [Abstract]; The protein expression of PDGF-A, PDGF-B, PDGF-C, and PDGF-D in hearts from mice treated with vehicle, Imatinib (IMA), ISO, IMA+ISO for one week is tested by Western blot.

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2017 Aug 6:23:3808-3816. [Abstract]; The kinase activity of c-Kit is enhanced in an animal model of cardiac fibrosis. The lysates of heart tissues from a mice model treated with vehicle, Imatinib (IMA), ISO, or Imatinib + ISO for one week are analyzed for phosphorylation level of p-c-Kit (Tyr719) and total protein level of c-Kit. The western blotting results from one mouse in each group and the statistical analysis of the western blotting bands are shown.

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118. [Abstract]; In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72. [Abstract]; Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.

: Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: J Bioenerg Biomembr. 2012 Feb;44(1):155-61. [Abstract]; Differences in sensitivity of PDR-mutants to 3-BP, Imatinib methanesulfonate, Daunorubicin and Rhodamine 6 G. Minimal medium (YNB) with sucrose.

Bcr-Abl アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Abl Bcr-Abl

PDGFR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PDGFR PDGFRβ PDGFRα

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

IC₅₀ & Target

IC50: ~100 nM (c-Kit, Bcr-Abl, and PDGFR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.87 3 Compound: Imatinib mesylate	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
A549	IC₅₀	1.87 3 Compound: Imatinib mesylate	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
A549	IC₅₀	1.87 3 Compound: Imatinib mesylate	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
Bel-7402	IC₅₀	55.52 3 Compound: Imatinib mesylate	Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
Bel-7402	IC₅₀	55.52 3 Compound: Imatinib mesylate	Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
Bel-7402	IC₅₀	55.52 3 Compound: Imatinib mesylate	Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
GIST882	IC₅₀	1.7 3 Compound: Gleevec	Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay	[PMID: 24900212]
GIST882	IC₅₀	1.7 3 Compound: Gleevec	Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay	[PMID: 24900212]
K562	EC₅₀	0.09 3 Compound: 1, Gleevec	Antiproliferative activity against K562 cells expressing Bcr-Abl Antiproliferative activity against K562 cells expressing Bcr-Abl	[PMID: 16678414]
GIST882	IC₅₀	1.7 3 Compound: Gleevec	Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay	[PMID: 24900212]
K562	IC₅₀	0.21 3 Compound: 1, gleevec	Cytotoxicity against human K562 cells after 24 hrs by MTT assay Cytotoxicity against human K562 cells after 24 hrs by MTT assay	[PMID: 22000207]
K562	IC₅₀	0.21 3 Compound: 1, gleevec	Cytotoxicity against human K562 cells after 24 hrs by MTT assay Cytotoxicity against human K562 cells after 24 hrs by MTT assay	[PMID: 22000207]
K562	IC₅₀	0.31 3 Compound: Imatinib mesylate	Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay	[PMID: 28075592]
K562	IC₅₀	0.31 3 Compound: Imatinib mesylate	Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay	[PMID: 28075592]
KBM5	IC₅₀	152.2 1 Compound: IM	Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
KU812 cell line	EC₅₀	0.6 3 Compound: Imatinib mesylate	Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 29778892]
KBM5	IC₅₀	310.6 1 Compound: IM	Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
MCF7	IC₅₀	0.83 3 Compound: 1, gleevec	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 22000207]
KU812 cell line	EC₅₀	0.6 3 Compound: Imatinib mesylate	Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 29778892]
KU812 cell line	IC₅₀	311.2 1 Compound: IM	Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
MDA-MB-231	IC₅₀	1.8 3 Compound: 1, gleevec	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 22000207]
K562	EC₅₀	0.09 3 Compound: 1, Gleevec	Antiproliferative activity against K562 cells expressing Bcr-Abl Antiproliferative activity against K562 cells expressing Bcr-Abl	[PMID: 16678414]
LAMA-84	IC₅₀	100 1 Compound: IM	Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 28523104]
LAMA-84	IC₅₀	100 1 Compound: IM	Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 28523104]
K562	IC₅₀	0.21 3 Compound: 1, gleevec	Cytotoxicity against human K562 cells after 24 hrs by MTT assay Cytotoxicity against human K562 cells after 24 hrs by MTT assay	[PMID: 22000207]
MKN-45	IC₅₀	12.18 3 Compound: Imatinib mesylate	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
MCF7	IC₅₀	0.83 3 Compound: 1, gleevec	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 22000207]
KBM5	IC₅₀	152.2 1 Compound: IM	Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
MDA-MB-231	IC₅₀	1.8 3 Compound: 1, gleevec	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 22000207]
K562	IC₅₀	0.31 3 Compound: Imatinib mesylate	Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay	[PMID: 28075592]
KBM5	IC₅₀	152.2 1 Compound: IM	Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
MKN-45	IC₅₀	12.18 3 Compound: Imatinib mesylate	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
KBM5	IC₅₀	310.6 1 Compound: IM	Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
KBM5	IC₅₀	310.6 1 Compound: IM	Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
KU812 cell line	IC₅₀	311.2 1 Compound: IM	Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
SGC-7901	IC₅₀	0.208 3 Compound: Imatinib mesylate	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
LAMA-84	IC₅₀	100 1 Compound: IM	Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 28523104]
SGC-7901	IC₅₀	0.208 3 Compound: Imatinib mesylate	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
Vero C1008	CC₅₀	> 30.86 3 Compound: Imatinib Mesylate	CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	CC₅₀	>30.86 3 Compound: Imatinib Mesylate	CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
LAMA-84	IC₅₀	100 1 Compound: IM	Antiproliferative activity against human LAMA-84 cells overexpressing BCR/ABL assessed as cell growth inhibition Antiproliferative activity against human LAMA-84 cells overexpressing BCR/ABL assessed as cell growth inhibition	[PMID: 28523104]
Vero C1008	CC₅₀	> 30.86 3 Compound: Imatinib Mesylate	CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	CC₅₀	>100 3 Compound: 13	Cytotoxicity against African green monkey Vero E6 cells Cytotoxicity against African green monkey Vero E6 cells	[PMID: 33539089]
Vero C1008	IC₅₀	3.24 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482
MCF7	IC₅₀	0.83 3 Compound: 1, gleevec	Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay	[PMID: 22000207]
MDA-MB-231	IC₅₀	1.8 3 Compound: 1, gleevec	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay	[PMID: 22000207]
Vero C1008	IC₅₀	5.32 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	IC₅₀	3.24 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	IC₅₀	5.32 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482
MKN-45	IC₅₀	12.18 3 Compound: Imatinib mesylate	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
SGC-7901	IC₅₀	0.208 3 Compound: Imatinib mesylate	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA	[PMID: 32866755]
Vero C1008	CC₅₀	> 100 3 Compound: 13	Cytotoxicity against African green monkey Vero E6 cells Cytotoxicity against African green monkey Vero E6 cells	[PMID: 33539089]
Vero C1008	CC₅₀	> 30.86 3 Compound: Imatinib Mesylate	CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	CC₅₀	> 30.86 3 Compound: Imatinib Mesylate	CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	IC₅₀	3.24 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482
Vero C1008	IC₅₀	5.32 3 Compound: Imatinib Mesylate	IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells	10.1101/2020.03.25.008482

体外実験

Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM^[1]. Imatinib (STI571) mesylate is very effective (in vitro IC₅₀ of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC₅₀, 410 nM) and PDGFR (in vitro IC₅₀, 380 nM)^[2]. Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC₅₀ of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2^[3]. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph⁺) acute lymphoblastic leukemia (ALL)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Animals treated with Imatinib Mesylate show a decrease of mean body weight throughout the whole study. Body weight loss is noticeable in mice from groups that receive chemotherapy and the vitamin D analog combined treatment. The body weight decrease of mice treat with both combined Imatinib mesylate and PRI-2191 is the highest (15%) on Day 22 of the experiment, but after that day, mice start to recover^[4]. In a rat Ischemia/reperfusion injury (IRI) model, Imatinib mesylate attenuates lung injury by an antipermeability and antiinflammatory effect. The delivery and function of Imatinib mesylate in the lung is also confirmed in this model^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

589.71

分子式

C₃₀H₃₅N₇O₄S

CAS 番号

220127-57-1

Appearance

Solid

Color

White to off-white

SMILES

O=S(O)(C)=O.O=C(NC1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 125 mg/mL (211.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 50 mg/mL (84.79 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6957 mL	8.4787 mL	16.9575 mL
5 mM	0.3391 mL	1.6957 mL	3.3915 mL
10 mM	0.1696 mL	0.8479 mL	1.6957 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (169.57 mM); Clear solution; Need ultrasonic
Protocol 2

Add each solvent one by one: Saline
Solubility: 100 mg/mL (169.57 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.97%

Select Batch:

データシート (278 KB) SDS (393 KB)

COA (243 KB) LCMS (262 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Heinrich MC, 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. [Content Brief]

[2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9. [Content Brief]

[3]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8 [Content Brief]

[4]. Maj E, et al. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13;16(11):27191-207. [Content Brief]

[5]. Tanaka S, et al. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Jul 23. pii: S0003-4975(16)30523-9 [Content Brief]

[6]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Content Brief]

細胞実験 ^[4]	Tested A549 cells are placed in 96-well flat-bottom plates at a density of 5×10³ cells per well 24 h before the addition of the test compounds. The cells are incubated for 96 h with two different concentrations (10 and 100 nM) of PRI-2191 and concurrently with various concentrations of Imatinib mesylate (10, 100, 1000 and 10,000 ng/mL) and other cytostatic drugs (Docetaxel (DTX) or Idarubicin (ID) : 0.1, 1, 10, 100 ng/mL; Cisplatin (CIS): 1, 10, 100, 1000 ng/mL). The sulforhodamine B (SRB) assay is performed to evaluate the cytotoxic effect. As a result, IC₅₀ is calculated for each separate experiment in Cheburator 0.4, Dmitry Nevozhay software^[4]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[4]^[5]	Mice^[4] NOD/SCID female mice, 12-16 weeks old, body weight of 20-25 g, are used. Mice are subcutaneously (s.c.) inoculated in the right flank of the abdomen with A549 tumor cells suspension (5×10⁶ cells in 0.2 mL of Hank’s medium per mouse, Day 0) and then are randomized into groups receiving varied combinations of vitamin D analogs and chemotherapeutics. One out of two experimental protocols is applied in the respective experiments: 1. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 75 mg/kg/day, daily for 19 days (from Days 7-25). PRI-2191 is administered s.c. or by oral gavage at a dose of 2 μg/kg/day, 3 times a week (on Days 7, 12, 14, 16, 19, 21 and 23). 2. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 50 mg/kg/day, daily for 13 days (from Days 7-19). PRI-2191 and PRI-2205 are administered s.c. at doses of 1 or 10 μg/kg/day, respectively, 3 times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24 and 26). At the end of the experiments, blood is collected under anesthesia; then, the mice are sacrificed. Rats^[5] Male Lewis rats weighing 270 to 320 g are used in the experiments. Imatinib mesylate (50 mg/kg) is injected intraperitoneally in the Imatinib group (n=7), and 0.5 mL of 20% DMSO without Imatinib is administered in the vehicle group (n=7). The dose of 25 mg/kg is preliminarily tested, and it produces a little improvement in lung function without statistical significance. The dose of 50 mg/kg and intraperitoneal administration are adopted based on this result and past reports. The animals undergo left thoracotomy, and the left hilum is occluded with a small metallic clamp. The occlusion is performed 20 minutes after Imatinib or vehicle administration. During clamping, the tidal volume (TV) and respiratory rate (RR) are adjusted to 8 mL/kg and 80 breaths/min, respectively. After 90 minutes of ischemia, the clamp is removed and reperfusion is maintained for 120 minutes. During reperfusion, blood flow and ventilation are restored in the bilateral lung. In the sham group (n=6), the animals are heparinized, thoracotomized, and ventilated for 210 minutes. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Heinrich MC, 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. [Content Brief] [2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9. [Content Brief] [3]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8 [Content Brief] [4]. Maj E, et al. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13;16(11):27191-207. [Content Brief] [5]. Tanaka S, et al. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Jul 23. pii: S0003-4975(16)30523-9 [Content Brief] [6]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.6957 mL	8.4787 mL	16.9575 mL	42.3937 mL
	5 mM	0.3391 mL	1.6957 mL	3.3915 mL	8.4787 mL
	10 mM	0.1696 mL	0.8479 mL	1.6957 mL	4.2394 mL
	15 mM	0.1130 mL	0.5652 mL	1.1305 mL	2.8262 mL
	20 mM	0.0848 mL	0.4239 mL	0.8479 mL	2.1197 mL
	25 mM	0.0678 mL	0.3391 mL	0.6783 mL	1.6957 mL
	30 mM	0.0565 mL	0.2826 mL	0.5652 mL	1.4131 mL
	40 mM	0.0424 mL	0.2120 mL	0.4239 mL	1.0598 mL
	50 mM	0.0339 mL	0.1696 mL	0.3391 mL	0.8479 mL
	60 mM	0.0283 mL	0.1413 mL	0.2826 mL	0.7066 mL
	80 mM	0.0212 mL	0.1060 mL	0.2120 mL	0.5299 mL
DMSO	100 mM	0.0170 mL	0.0848 mL	0.1696 mL	0.4239 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Imatinib Mesylate Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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イマチニブメシル酸塩 (Synonyms: Imatinib (Mesylate); STI571 (Mesylate); CGP-57148B (Mesylate))

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純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Imatinib Mesylate Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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イマチニブメシル酸塩 (Synonyms: Imatinib (Mesylate); STI571 (Mesylate); CGP-57148B (Mesylate))

カスタマーレビュー

Other Forms of Imatinib Mesylate:

イマチニブメシル酸塩 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

Bcr-Abl アイソフォーム固有の製品をすべて表示:

PDGFR アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

イマチニブメシル酸塩 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Imatinib Mesylate Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report

イマチニブメシル酸塩関連抗体

イマチニブメシル酸塩関連抗体