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ZM 336372

Cat. No. M1818
ZM 336372 Structure
Synonym:

ZM336372

Size Price Availability Quantity
10mg USD 105 In stock
50mg USD 360 In stock
100mg USD 480 In stock
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Quality Control
Biological Activity

ZM 336372 is a potent, selective ATP-competitive inhibitor of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf). The Ras/Raf-1 signalling pathway is a well-characterized system that links receptor tyrosine kinase (RTK) activation with changes in gene expression and cell behavior. Raf-1 is a serine/threonine protein kinase that phosphorylates and activates MAPK-kinase (MEK) in response to activation by Ras. ZM 336372 also inhibits SAPK2/p38 (IC50 = 2 μM). Selective over 17 other protein kinases including PKA, PKC, p42 MAPK, CDK1 and SAPK1/JNK (up to 50 μM). ZM 336372 causes growth inhibition, suppression of hormone secretion, and up-regulation of cell cycle inhibitors in a human hepatocellular carcinoma cell line.

Protocol
Cell Experiment
Cell lines H727 and BON cells
Preparation method Cell Proliferation Assay
Proliferation of H727 and BON cells after treatment with ZM336372 was measured using a 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (Sigma). Cells were trypsinized and plated in triplicate to 24-well plates and allowed to adhere overnight. Then, cells were treated with either 100 μmol/L ZM336372 or DMSO (2%) and incubated. Media were changed every 2 days with new treatment. At each time point, cell growth rates were analyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to the cultured cells following manufacturer's instructions. Absorbance was determined using spectrophotometer at a wavelength of 540 nm.
Concentrations 100 μmol/L
Incubation time 10 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
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 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.

Chemical Information
Molecular Weight 389.45
Formula C23H23N3O3
CAS Number 208260-29-1
Purity >99%
Solubility DMSO ≥78 mg/mL
Storage at -20°C
References

ZM336372, a Raf-1 activator, causes suppression of proliferation in a human hepatocellular carcinoma cell line.
Deming D, et al. J Gastrointest Surg. 2008 May;12(5):852-7. PMID: 18299943.

ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells.
Van Gompel JJ, et al. Mol Cancer Ther. 2005 Jun;4(6):910-7. PMID: 15956248.

Paradoxical activation of Raf by a novel Raf inhibitor.
Hall-Jackson CA, et al. Chem Biol. 1999 Aug;6(8):559-68. PMID: 10421767.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ZM 336372, ZM336372 supplier, Raf, inhibitors

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