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APG-2575 (lisaftoclax) Bcl-2 inhibitor

Name: APG-2575 (lisaftoclax)
Brand: Selleck Chemicals
SKU: S9970
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9970

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.

Chemical Structure

Molecular Weight: 882.43

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.55

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Chemical Information, Storage & Stability

Molecular Weight	882.43	Formula	C₄₅H₄₈ClN₇O₈S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2180923-05-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.650mg/ml (1.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (0.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	Bcl-2 ^[1] 2 nM Bcl-xl ^[1] 5.9 nM
References	https://www.freepatentsonline.com/WO2018027097A1.html

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

Tech Support

Handling Instructions

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