Imatinib Mesylate (STI571)

Catalog No.S1026

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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Imatinib Mesylate (STI571) Chemical Structure

Imatinib Mesylate (STI571) Chemical Structure
Molecular Weight: 589.71

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Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
T47D NXL1NIFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWnuN3hYUUN3ME21NEDPxE1?M3SxblI2QDZ|MkOy
Hep G2M3ThbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3vPeWlEPTB;M{Gg{txOMWOyOVg3OzJ|Mh?=
DU145NFLyOWZE\WyuIG\pZYJqdGm2eTDBd5NigQ>?MYeyNQKBkc7:TR?=MWe2MVczKGh?NHuzXZpl\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdIm=NV:4dVc2OjV5OE[2OVY>
PC3 NI\OOGFE\WyuIG\pZYJqdGm2eTDBd5NigQ>?NH\MXo4zOOLCid88US=>M2G0OFYuPzJiaB?=MYDpcoNz\WG|ZYOgZ4VtdCC4aXHibYxqfHl?MWGyOVc5PjZ3Nh?=
DU145NVnkTGJJSXCxcITvd4l{KEG|c3H5MVmyNQKBkc7:TR?=MV20PE84OiCqMoPsbY5lfWOnczDj[YxtKGSnYYToJIJ6KGGyb4D0c5Nqew>?NXvTNZk1OjV5OE[2OVY>
PC3 NWPVfG1OSXCxcITvd4l{KEG|c3H5MkPzNlDjiIoQvF2=MorSOFgwPzJiaB?=MmWwbY5kemWjc3XzJINmdGxic4Xyeol3[Wx?MnTkNlU4QDZ4NU[=
MCF-7NXPIOGJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NYry[I9uOTBizszNMYG0PEBpNHnEPYtjdG:la4OgZ4VtdCCycn;sbYZmemG2aX;uJIlv[3KnYYPlJIlv\HWlZXSgZpkhSkp|Wh?=M3HwPFI2Ojd2MEO0
K-562 M1[xNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MofjTWM2OD1zIN88US=>NHjwW4IzPTJ|OU[2Ni=>
K562 M1T6O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXXJR|UxRTBwNdMg{txONGHiUIczPDl|OUSxPC=>
K562rNHnCW4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2nRVmlEPTB;MUFCpO69VQ>?M2LxUFI1QTN7NEG4
K562NX\YcHkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MXLFR|UxRTBwMEmg{txOMX6xOlY4QDRzNB?=
K562MWDDfZRwfG:6aXPpeJkhSXO|YYm=M2L0e|I1KGh?M{TibGlEPTB;MD6yNUDPxE1?NYq3R2hDOjJyMECyNFc>
MCF-7M{XOfWN6fG:2b4jpZ4l1gSCDc4PhfS=>M2\VNlI1KGh?M4jKWmlEPTB;MD64N{DPxE1?M{PJfFIzODByMkC3
MDA-MB-23Mli4R5l1d3SxeHnjbZR6KEG|c3H5NYe4SHpJOjRiaB?=MWDJR|UxRTFwODFOwG0>Mlq2NlIxODB{MEe=
GIST882MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2mxTlk3KGh?MWrJR|UxRTFwNzFOwG0>NX3iXXhbOjR7MECyNVI>

... 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [3]

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.

Animal Study: [5]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Buchdunger E, et al. Proc Natl Acad Sci USA, 1995, 92(7), 2558–2562.

[2] Heinrich MC, et al. Blood. 2000, 96(3), 925-932.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02709083 Not yet recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University December 2016 Phase 2
NCT02812693 Not yet recruiting Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma|Stage IV Skin Melanoma Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|O  ...more Joanne Jeter|National Cancer Institute (NCI)|Merck Ltd.|Ohio State University Comprehensive Cancer Center September 2016 Phase 1|Phase 2
NCT02538926 Not yet recruiting B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T  ...more B Acute Lymphoblastic Leukemia|B Lymphoblastic Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent B Lymphoblastic Lymphoma|Recurrent T Lymphoblastic Leukemia/Lymphoma|Refractory B Lymphoblastic Lymphoma|Refractory T Lymphoblastic Lymphoma|T Acute Lymphoblastic Leukemia|T Lymphoblastic Lymphoma University of Washington|National Cancer Institute (NCI) August 2016 Phase 2
NCT02687425 Not yet recruiting Leukemia, Myelogenous, Chronic, BCR-ABL Positive Meng Li|Tongji Hospital February 2016 Phase 2
NCT02712112 Recruiting Gastrointestinal Stromal Tumors (GISTs) Asan Medical Center January 2016 Phase 2

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Chemical Information

Download Imatinib Mesylate (STI571) SDF
Molecular Weight (MW) 589.71
Formula

C29H31N7O.CH4SO3

CAS No. 220127-57-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CGP-57148B, ST-1571 Mesylate
Solubility (25°C) * In vitro DMSO 118 mg/mL (200.09 mM)
Water 118 mg/mL (200.09 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide methanesulfonic acid

Tech Support

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