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Imatinib

Cat. No. M3241
Imatinib Structure
Synonym:

STI571

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
100mg USD 36  USD40 In stock
200mg USD 48.6  USD54 In stock
500mg USD 77.4  USD86 In stock
1g USD 109.8  USD122 In stock
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Quality Control
Biological Activity

Imatinib is a number of tyrosine kinase enzymes specific inhibitor. It act by specifically inhibiting a certain enzyme that is characteristic of a particular cancer cell, rather than non-specifically inhibiting and killing all rapidly dividing cells, and served as a model for other targeted therapy modalities through tyrosine kinase inhibition. In chronic myelogenous leukemia, the Philadelphia chromosome leads to a fusion protein of abl with bcr (breakpoint cluster region), termed bcr-abl. As this is now a constitutively active tyrosine kinase, it is used to decrease bcr-abl activity. It is being used as an experimental agent to suppress platelet-derived growth factor (PDGF) by inhibiting its receptor (PDGF-Rβ).

Product Citations
Protocol
Cell Experiment
Cell lines BON-1 cells and NCI-H727 cells
Preparation method Seeding BON-1 cells and NCI-H727 cells into flat-bottomed 96-well plates in triplicate and allowing 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. Determing the number of metabolically active cells by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and measuring absorbance in a Packard Spectra microplate reader at 540 nm.after 48 hours (control cultures do not reach confluence), calculating growth inhibition 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.
Concentrations ~100 μM
Incubation time 48 hours
Animal Experiment
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)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 493.6
Formula C29H31N7O
CAS Number 152459-95-5
Purity 99.48%
Solubility DMSO 5 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Imatinib, STI571 supplier, c-Kit, inhibitors

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