Amcasertib (BBI503)

Catalog No.S8572

For research use only.

Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity.

Amcasertib (BBI503) Chemical Structure

CAS No. 1129403-56-0

Selleck's Amcasertib (BBI503) has been cited by 3 Publications

Purity & Quality Control

Choose Selective Stemness kinase Inhibitors

Biological Activity

Description Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity.
Targets
Nanog [1]
In vitro

BBI-503 is orally-administered compound, which is designed to target CSC pathways in multiple tumour types[1].

In vivo BBI503 inhibits Nanog and other cancer stem cell pathways by targeting kinases, and shows encouraging early signs of anti-cancer activity for patients with advanced colorectal cancer[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 539.69
Formula

C31H33N5O2S

CAS No. 1129403-56-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)C4=CSC(=N4)C5=CC=CC=C5)NC2=O)C

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02232620 Terminated Drug: BBI503 Gastrointestinal Stromal Tumors Sumitomo Pharma Oncology Inc. March 13 2017 Phase 2
NCT02232646 Withdrawn Drug: BBI503 Urologic Malignancies|Renal Cell Carcinoma|Urothelial Carcinoma Sumitomo Pharma Oncology Inc. January 2017 Phase 2
NCT02432326 Completed Drug: BBI608|Drug: BBI503 Cancer|Advanced Solid Tumors Sumitomo Pharma Oncology Inc. April 2015 Phase 1
NCT02354898 Completed Drug: BBI503|Drug: Sorafenib Advanced Solid Tumors|Hepatocellular Carcinoma Sumitomo Pharma Co. Ltd. March 2015 Phase 1
NCT02232633 Completed Drug: BBI503 Hepatocellular Carcinoma|Cholangiocarcinoma Sumitomo Pharma Oncology Inc. February 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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