1. Apoptosis
  2. Bcl-2 Family
  3. Lisaftoclax

Lisaftoclax  (Synonyms: APG-2575; Bcl-2/Bcl-xl inhibitor 1)

Art. -Nr.: HY-129179 Reinheit: 99.78%
Handling Instructions Technical Support

Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.

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Lisaftoclax

Lisaftoclax Chemische Struktur

CAS. Nr. : 2180923-05-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 1 publication(s) in Google Scholar

Other Forms of Lisaftoclax:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lisaftoclax

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Beschreibung

Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively[1].

IC50 & Target[1]

Bcl-2

2 nM (IC50)

Bcl-xL

5.9 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
RS4-11 IC50
161 1
Compound: 3; APG-2575
Inhibition of cell growth in human RS4-11 cells harboring Bcl-2 G101V mutant incubated for 2 days by CellTiter-Glo luminescent cell viability assay
Inhibition of cell growth in human RS4-11 cells harboring Bcl-2 G101V mutant incubated for 2 days by CellTiter-Glo luminescent cell viability assay
[PMID: 38695063]
RS4-11 IC50
6.3 1
Compound: 3; APG-2575
Inhibition of cell growth in human RS4-11 cells incubated for 2 days by CellTiter-Glo luminescent cell viability assay
Inhibition of cell growth in human RS4-11 cells incubated for 2 days by CellTiter-Glo luminescent cell viability assay
[PMID: 38695063]
In Vitro

Lisaftoclax (compound 6) exhibits IC50 values of 5.5 nM and 6.4 nM in Bcl-2 dependent RS4;11 cells and Bcl-xl dependent Molm13 cells[1].

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

Klinische Studie
Molekulargewicht

882.42

Formel

C45H48ClN7O8S

CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NS(=O)(C1=CC=C(NC[C@@H]2OCCOC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC(CC5)=C(C6=CC=C(Cl)C=C6)CC75CCC7)CC4)C=C3OC8=CN=C(NC=C9)C9=C8

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (113.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1332 mL 5.6662 mL 11.3325 mL
5 mM 0.2266 mL 1.1332 mL 2.2665 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (2.83 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.78%

Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1332 mL 5.6662 mL 11.3325 mL 28.3312 mL
5 mM 0.2266 mL 1.1332 mL 2.2665 mL 5.6662 mL
10 mM 0.1133 mL 0.5666 mL 1.1332 mL 2.8331 mL
15 mM 0.0755 mL 0.3777 mL 0.7555 mL 1.8887 mL
20 mM 0.0567 mL 0.2833 mL 0.5666 mL 1.4166 mL
25 mM 0.0453 mL 0.2266 mL 0.4533 mL 1.1332 mL
30 mM 0.0378 mL 0.1889 mL 0.3777 mL 0.9444 mL
40 mM 0.0283 mL 0.1417 mL 0.2833 mL 0.7083 mL
50 mM 0.0227 mL 0.1133 mL 0.2266 mL 0.5666 mL
60 mM 0.0189 mL 0.0944 mL 0.1889 mL 0.4722 mL
80 mM 0.0142 mL 0.0708 mL 0.1417 mL 0.3541 mL
100 mM 0.0113 mL 0.0567 mL 0.1133 mL 0.2833 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Lisaftoclax
Art. -Nr.:
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