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APG-2575 (lisaftoclax)

Name: APG-2575 (lisaftoclax)
Brand: Selleck Chemicals
SKU: S9970

Catalog No.S9970 Purity: 99.55%

APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.

APG-2575 (lisaftoclax) Chemical Structure

CAS: 2180923-05-9

Purity & Quality Control

Batch: S997001 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.55%

99.55

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Biological Activity

Description

APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.

Targets

Bcl-2 ^[1]	Bcl-xl ^[1]
2 nM	5.9 nM

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06182969	Not yet recruiting	SLE	Ascentage Pharma Group Inc.\|Suzhou Yasheng Pharmaceutical Co. Ltd.	December 2023	Phase 1\|Phase 2
NCT05495035	Recruiting	Lymphoblastic Leukemia Acute Childhood\|Leukemia Lymphoblastic Acute Philadelphia-Positive\|Relapsed Leukemia\|Refractory Leukemia	Institute of Hematology & Blood Diseases Hospital China	September 1 2022	Phase 1
NCT04496349	Recruiting	T-Prolymphocytic Leukemia	Ascentage Pharma Group Inc.	July 12 2021	Phase 2
NCT04494503	Recruiting	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	Ascentage Pharma Group Inc.	August 31 2020	Phase 1\|Phase 2
NCT03913949	Active not recruiting	Chronic Lymphocytic Leukemia\|Non Hodgkin Lymphoma	Ascentage Pharma Group Inc.\|Suzhou Yasheng Pharmaceutical Co. Ltd.	June 3 2019	Phase 1
NCT03537482	Recruiting	Hematologic Malignancies	Ascentage Pharma Group Inc.	August 7 2018	Early Phase 1

References

[1] WANG, Chia, et al. WO2018027097A1.

Chemical lnformation & Solubility

Molecular Weight	882.43	Formula	C₄₅H₄₈ClN₇O₈S
CAS No.	2180923-05-9	SDF	--
Smiles	ClC1=CC=C(C=C1)C2=C(CCC3(CCC3)C2)CN4CCN(CC4)C5=CC(=C(C=C5)C(=O)N[S;v6](=O)(=O)C6=CC(=C(NCC7COCCO7)C=C6)[N;v5](=O)=O)OC8=CN=C9[NH]C=CC9=C8
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (113.32 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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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