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Aderbasib

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Catalog No. T40901Cas No. 791828-58-5
Alias INCB7839, INCB007839

Aderbasib (INCB007839) is a highly potent and orally active hydroxamate-based inhibitor of ADAM10 and ADAM17, with low nanomolar affinity. This compound demonstrates strong antineoplastic activity and holds potential for cancer research in various areas, such as diffuse large B-cell non-Hodgkin lymphoma, HER2-positive breast cancer, gliomas, and more.

Aderbasib

Aderbasib

😃Good
Catalog No. T40901Alias INCB7839, INCB007839Cas No. 791828-58-5
Aderbasib (INCB007839) is a highly potent and orally active hydroxamate-based inhibitor of ADAM10 and ADAM17, with low nanomolar affinity. This compound demonstrates strong antineoplastic activity and holds potential for cancer research in various areas, such as diffuse large B-cell non-Hodgkin lymphoma, HER2-positive breast cancer, gliomas, and more.
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1 mg297 â‚¬7-10 days
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Product Introduction

Bioactivity
Description
Aderbasib (INCB007839) is a highly potent and orally active hydroxamate-based inhibitor of ADAM10 and ADAM17, with low nanomolar affinity. This compound demonstrates strong antineoplastic activity and holds potential for cancer research in various areas, such as diffuse large B-cell non-Hodgkin lymphoma, HER2-positive breast cancer, gliomas, and more.
In vitro
Aderbasib acts by inhibiting metalloprotease activity, specifically binding to the active site within the metalloproteinase domain. At concentrations ranging from 10-100 μM, Aderbasib reduces the interaction between ADAM17 and sE2-Fc; notably, this interaction decreases as Aderbasib concentration increases, leading to a substantial reduction in sE2-Fc binding at 100 μM in trypsinized PK15 cells[2]. Additionally, when pre-treated for 0.5 h, Aderbasib displays an antiviral effect against CSFV pseudovirus at both 100 μM and 1 mM concentrations in PK15 cells[2].
In vivo
Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week for 2 weeks starting from the fourth week) effectively inhibits the growth of glioma in SU-pcGBM2 NSG mouse xenografts[1]. Prepared as an injection solution with 2% DMSO, 2% Tween 80, 48% PEG300, and 48% water, Aderbasib significantly suppresses pediatric glioblastoma orthotopic xenografts in NSG mice at a 50 mg/kg dosage following the specified schedule[1]. This data is for academic reference only.
AliasINCB7839, INCB007839
Chemical Properties
Molecular Weight416.47
FormulaC21H28N4O5
Cas No.791828-58-5
Relative Density.1.38 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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