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LY2784544 (Gandotinib)

Cat. No. M3535
LY2784544 (Gandotinib) Structure
Synonym:

gandotinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 117  USD130 In stock
2mg USD 63  USD70 In stock
5mg USD 115.2  USD128 In stock
10mg USD 169.2  USD188 In stock
50mg USD 630  USD700 In stock
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Quality Control
Biological Activity

LY2784544 is a small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM. The antiproliferative activity of LY2784544 and its ability to induce apoptosis were examined by Celltiter-Glo Cell Viability and Caspase-Glo 3/7 Apoptosis Assays, respectively.? In the in vitro tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, it potently inhibited the JAK2 V617F-STAT5 signaling at a concentration that was 41-fold lower than that required to inhibit IL-3-activated wild type JAK2-STAT5 signaling (IC50 = 0.055 uM for JAK2 V617F vs. 2.26 uM for WT JAK2). Similarly in the proliferation assay, LY2784544 selectively inhibited the JAK2 V617F-driven cell proliferation (IC50= 0.068 uM). Inhibition of JAK2 V617F signaling correlated well with the induction of apoptosis (EC50= 0.113 uM) in Ba/F3 cell model.

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2015). Figure 3. LY2784544
Method Viral knockdown
Cell Lines MCF10A cells
Concentrations 1.25 μmol/L
Incubation Time 48 h
Results Using the xCELLigence system to monitor cell growth in real time, LY2784544 had only a modest effect on MCF10A cells at 0.32, 0.63, and 1.25 μmol/L concentrations; however, the cell proliferation index was reduced in the CDH1-/- cells in a concentration-dependent manner.
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 469.94
Formula C23H25ClFN7O
CAS Number 1229236-86-5
Purity >99%
Solubility DMSO 54 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2784544 (Gandotinib), gandotinib supplier, JAK, inhibitors

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