1. Metabolic Enzyme/Protease
  2. MMP
  3. Aderbasib

Aderbasib (Synonyms: INCB007839; INCB7839)

Cat. No.: HY-10293
Handling Instructions

Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al.

For research use only. We do not sell to patients.

Aderbasib Chemical Structure

Aderbasib Chemical Structure

CAS No. : 791828-58-5

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Description

Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al[1].

IC50 & Target[1]

ADAM10

 

ADAM17

 

In Vitro

Aderbasib inhibits the metalloprotease activity through binding to the active site of the metalloproteinase domain. Aderbasib (10-100 μM) inhibits the interaction between ADAM17 and sE2-Fc, as the concentration of the compound increases, binding of sE2-Fc decreased accordingly, with almost no binding detected at 100 μM in trypsinized PK15 cells[2].
Aderbasib (100-1000μM; pre-treated for 0.5 h) shows antiviral effect against CSFV pseudovirus at 100 μM and 1 mM in PK15 cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Aderbasib (intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks) blocks glioma growth of SU-pcGBM2 NSG mice xenografts[1].
INCB7839 can be formulated in 2% DMSO, 2% Tween 80, 48% PEG300, 48% water as a injection solution. This is for literature reference only[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NSG mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 50 mg/kg; 5 days per week beginning four weeks; 2 weeks
Result: Robustly inhibited growth of pediatric glioblastoma orthotopic xenografts.
Molecular Weight

416.47

Formula

C₂₁H₂₈N₄O₅

CAS No.
SMILES

O=C(N(CC1)CCN1C2=CC=CC=C2)[[email protected]]([[email protected]](C3)C(NO)=O)N(CC43CC4)C(OC)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

AderbasibINCB007839 INCB7839INCB 007839INCB-007839INCB7839INCB 7839INCB-7839MMPMatrix metalloproteinasesB-cellnon-Hodgkin lymphomaHigh-grade gliomasHGGHER2+Inhibitorinhibitorinhibit

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