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ASP3026

Cat. No. M1950
ASP3026 Structure
Size Price Availability Quantity
10mg USD 115 In stock
50mg USD 350 In stock
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Quality Control
Biological Activity

ASP3026 is a potent ALK (Anaplastic Lymphoma Kinase) inhibitor. ASP3026 inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel. In an anchorage independent in vitro cell growth assay, ASP3026 inhibited the growth of NCI-H2228, a human NSCLC tumor cell line endogenously expressing EML4-ALK variant 3 and that of 3T3 cells expressing EML4-ALK variant 1, 2 and 3. The plasma and tumor concentrations of ASP3026 in mice xenografted with NCI-H2228 tumor were determined using high-performance liquid chromatography-tandem mass spectrometry. ASP3026 showed potent anti-tumor effects while crizotinib was ineffective even at 100 mg/gk qd in an EML4-ALK driven tumor model with gatekeeper mutation.

Protocol
Cell Experiment
Cell lines NPM-ALK+ ALCL cells Karpas 299, SR-786 and SU-DHL-1 cells
Preparation method MTS assay
Cell viability was measured using MTS reagent (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium; Promega, Madison, WI). Briefly, 1 × 105 cells were seeded into 96-well plates, and 20 μL of MTS reagent was added to each well and incubated for approximately 2 h at 37°C in 5% CO2. Plates were read at 490 nm.
Concentrations 0.1, 0.5 and 1 μ M
Incubation time 48 or 72 h
Animal Experiment
Animal models Systemic xenograft NPM-ALK+ ALCL model
Formulation 0.5% methylcellulose
Dosages 30 mg/kg daily for 12 weeks
Administration oral gavage
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 580.76
Formula C29H40N8O3S
CAS Number 1097917-15-1
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

The ALK inhibitor ASP3026 eradicates NPM-ALK⁺ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model.
George SK, et al. Oncotarget. 2014 Jul 30;5(14):5750-63. PMID: 25026277.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ASP3026 supplier, ALK, inhibitors

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