Amcasertib (BBI503)

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

Amcasertib (BBI503) Chemical Structure

CAS: 1129403-56-0

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

Purity & Quality Control

Batch: S857201 DMSO] 14 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.16%
99.16

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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
In vitro BBI-503 is orally-administered compound, which is designed to target CSC pathways in multiple tumour types[1].
In Vivo
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02232620 Terminated
Gastrointestinal Stromal Tumors
Sumitomo Pharma America Inc.
March 13 2017 Phase 2
NCT02232646 Withdrawn
Urologic Malignancies|Renal Cell Carcinoma|Urothelial Carcinoma
Sumitomo Pharma America Inc.
January 2017 Phase 2
NCT02432326 Completed
Cancer|Advanced Solid Tumors
Sumitomo Pharma America Inc.
April 2015 Phase 1
NCT02354898 Completed
Advanced Solid Tumors|Hepatocellular Carcinoma
Sumitomo Pharma Co. Ltd.
March 2015 Phase 1
NCT02232633 Completed
Hepatocellular Carcinoma|Cholangiocarcinoma
Sumitomo Pharma America Inc.
February 2015 Phase 2

Chemical Information & Solubility

Molecular Weight 539.69 Formula

C31H33N5O2S

CAS No. 1129403-56-0 SDF Download Amcasertib (BBI503) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 14 mg/mL ( (25.94 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

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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