[CAS NO. 1235034-55-5]  A-1155463

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PRODUCTS SPECIFICATIONS [1235034-55-5]

Catalog
HY-19725
Brand
MCE
CAS
1235034-55-5

DESCRIPTION [1235034-55-5]

Overview

MDLMFCD29924714
Molecular Weight669.79
Molecular FormulaC35H32FN5O4S2
SMILESO=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O

For research use only. We do not sell to patients.


Summary

A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC 50 of 70 nM in Molt-4 cell.


IC50 & Target

Bcl-xL

0.01 nM (Ki)

Bcl-2

80 nM (Ki)


In Vitro

A-1155463 shows picomolar binding affinity to BCL-X L (K i <0.01 nM), and >1000-fold weaker binding to BCL-2 (K i = 80 nM) and related proteins BCL-W (K i = 19 nM) and MCL-1 (K i > 440 nM) [2] . A-1155463 demonstrates strong growth inhibition of over half of the colorectal cell lines as defined by EC 50 values ≤0.5 μM in the presence of 10 % FBS [3] .

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


In Vivo

A-1155463 caused a mechanism-based and reversible thrombocytopenia in mice and inhibited H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses [2] .

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


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL ( 18.66 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4930 mL 7.4650 mL 14.9301 mL
5 mM 0.2986 mL 1.4930 mL 2.9860 mL
10 mM 0.1493 mL 0.7465 mL 1.4930 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: 1.25 mg/mL (1.87 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: 1.25 mg/mL (1.87 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: 1.25 mg/mL (1.87 mM); Clear solution; Need ultrasonic

* All of the co-solvents are available by MCE.