Imatinib Mesylate (STI571)

Catalog No.S1026 Synonyms: CGP-57148B, ST-1571 Mesylate

Imatinib Mesylate (STI571) Chemical Structure

Molecular Weight(MW): 589.71

Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

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In DMSO USD 191 In stock
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Cited by 38 Publications

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Biological Activity

Description Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.
Targets
PDGFR [1]
(Cell-free assay)		 c-Kit [2]
(M-07e cells)		 v-Abl [1]
(Cell-free assay)
100 nM 100 nM 600 nM
In vitro

In vitro assays for inhibition of a panel of tyrosine and serine/threonine protein kinases show that Imatinib inhibits the v-Abl tyrosine kinase and PDGFR potently with an IC50 of 0.6 and 0.1 μM, respectively. [1] Imatinib inhibits the SLF-dependent activation of wild-type c-kit kinase activity with a IC50 for these effects of approximately 0.1 μM, which is similar to the concentration required for inhibition of PDGFR. [2] Imatinib exhibits growth-inhibitory activity on the human bronchial carcinoid cell line NCI-H727 and the human pancreatic carcinoid cell line BON-1 with an IC50 of 32.4 and 32.8 μM, respectively. [3] A recent study shows that Imatinib has the potential to exert its antileukemia effects in chronic myelogenous leukemia by down-regulating hERG1 K(+) channels, which are highly expressed in leukemia cells and appear of exceptional importance in favoring leukemogenesis. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D  NVvSW2FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn[zTWM2OD13MDFOwG0> NVL5VJhNOjV6NkOyN|I>
Hep G2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTEUXVKSzVyPUOxJO69VQ>? MWKyOVg3OzJ|Mh?=
DU145 NUjsO2k{S2WubDDWbYFjcWyrdImgRZN{[Xl? NX7yeHVIOjEkgJpOwG0> NGPP[Ig3NTd{IHi= MljF[IVkemWjc3XzJINmdGxidnnhZoltcXS7 NE\6OJAzPTd6Nk[1Oi=>
PC3  MmX2R4VtdCCYaXHibYxqfHliQYPzZZk> NILUOW8zOOLCid88US=> NFzaZYk3NTd{IHi= MonFbY5kemWjc3XzJINmdGxidnnhZoltcXS7 M17GdFI2Pzh4NkW2
DU145 NXrsVY1pSXCxcITvd4l{KEG|c3H5 MoP0NlDjiIoQvF2= MWm0PE84OiCq MV\pcoR2[2W|IHPlcIwh\GWjdHigZpkh[XCxcITvd4l{ MkTnNlU4QDZ4NU[=
PC3  M4nSTGFxd3C2b4Ppd{BCe3OjeR?= MXqyNQKBkc7:TR?= MlfGOFgwPzJiaB?= NED2b4dqdmO{ZXHz[ZMh[2WubDDzeZJ3cX[jbB?= MkjjNlU4QDZ4NU[=
MCF-7 M2TtRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKxNEDPxE1? MkezOFghcA>? MX3icI9kc3NiY3XscEBxem:uaX\ldoF1cW:wIHnuZ5Jm[XOnIHnu[JVk\WRiYomgRmo{Yg>? NEf6Z3QzPTJ5NECzOC=>
K-562  NYr4XXJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXITWM2OD1zIN88US=> M3qze|I2OjN7Nk[y
K562  M3HRRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnkO3BpUUN3ME2wMlXDqM7:TR?= NIP6c48zPDl|OUSxPC=>
K562r NWPVR2VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELuXXVKSzVyPUGwxsDPxE1? MmntNlQ6Ozl2MUi=
K562 NV\ONmZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonVSWM2OD1yLkC5JO69VQ>? Moq0NVY3Pzh2MUS=
K562 M2frRmN6fG:2b4jpZ4l1gSCDc4PhfS=> NFr5WGIzPCCq NXr3[4tFUUN3ME2wMlIyKM7:TR?= NX3mSJVROjJyMECyNFc>
MCF-7 M2nRO2N6fG:2b4jpZ4l1gSCDc4PhfS=> MoT6NlQhcA>? NV\xdWpJUUN3ME2wMlg{KM7:TR?= NYXuRXZtOjJyMECyNFc>
MDA-MB-23 M2m2OmN6fG:2b4jpZ4l1gSCDc4PhfS=> NGTYZnIzPCCq MnnITWM2OD1zLkig{txO NUXi[pBHOjJyMECyNFc>
GIST882 NGDHSGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vFRVk3KGh? M3X4PGlEPTB;MT63JO69VQ>? MlP6NlQ6ODB{MUK=

... Click to View More Cell Line Experimental Data
In vivo Imatinib produces a different antitumor effect on three xenografted tumors derived from surgical samples of fresh human small cell lung cancers, with 80%, 40% and 78% growth inhibition of SCLC6, SCLC61 and SCLC108 tumors, respectively, and no significant inhibition of SCLC74 growth. [5] In high fat fed ApoE(-/-) mice, Imatinib significantly reduces the high fat-induced lipid staining area by 30%, 27% and 35% compared to high-fat diet untreated controls when dosed by gavage at 10, 20 and 40 mg/kg, respectively, and suppresses carotid artery lipid accumulation. [6]

Protocol

Kinase Assay:[1]
+ Expand

PDGF receptor kinase activity:

PDGF receptor is immunoprecipitated from BALB/c 3T3 cell extracts with rabbit antiserum to the murine PDGF receptor for 2 hours on ice. Protein A-Sepharose beads are used to collect the antigen-antibody complexes. The immunoprecipitates are washed twice with TNET (50 mM Tris, pH 7.5, 140 mM NaCl, 5 mM EDTA, 1% Triton X-100), once with TNE (50 mM Tris, pH 7.5, 140 mM EDTA), and once with kinase buffer (20 mM Tris, pH 7.5,10 mM MgCl2). After stimulation with PDGF (50 ng/mL) for 10 minutes at 4 °C, different concentrations of drug are added to the reaction mixture. PDGF receptor kinase activity is determined by incubation with 10 μCi [7-33P]-ATP and l μM ATP for 10 minutes at 4 °C. Immune complexes are separated by SDS-PAGE on 7.5% gels.
Cell Research:[3]
+ Expand
  • Cell lines: BON-1 cells and NCI-H727 cells
  • Concentrations: ~100 μM
  • Incubation Time: 48 hours
  • Method: BON-1 cells and NCI-H727 cells are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 hours (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated using the following formula: inhibition rate = (1 − a / b) × 100%, where a and b are the absorbance values of the treated and control groups, respectively.
    (Only for Reference)
Animal Research:[5]
+ Expand
  • Animal Models: SCLC6, SCLC61, SCLC 74 and SCLC108 small cell lung cancers are injected into Swiss mice (nu/nu, female).
  • Formulation: Imatinib is diluted in water.
  • Dosages: 70 or 100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 589.71
Formula

C29H31N7O.CH4SO3
CAS No. 220127-57-1
Storage powder
in solvent
Synonyms CGP-57148B, ST-1571 Mesylate

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03674099 Recruiting Multiple Sclerosis Tomas Olsson|The Swedish Research Council|Karolinska Institutet October 1 2018 Phase 2
NCT03516279 Recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group October 3 2018 Phase 2
NCT03674099 Recruiting Multiple Sclerosis Tomas Olsson|The Swedish Research Council|Karolinska Institutet October 1 2018 Phase 2
NCT03516279 Recruiting Chronic Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Minimal Residual Disease ECOG-ACRIN Cancer Research Group|National Cancer Institute (NCI)|Eastern Cooperative Oncology Group October 3 2018 Phase 2
NCT03688568 Recruiting Neurofibroma Plexiform Indiana University|Food and Drug Administration (FDA) September 1 2018 Phase 2
NCT03688568 Recruiting Neurofibroma Plexiform Indiana University|Food and Drug Administration (FDA) September 1 2018 Phase 2

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID