Venetoclax Powder CAS 1257044-40-8

ABT-199 Introduction

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Venetoclax powder (CAS 1257044-40-8, also known as ABT-199 or GDC-0199) is a highly selective inhibitor of Bcl-2 protein. Molecular formula: C45H50ClN7O7S Molecular weight: 868.44; EINECS Number: 820-130-9.Its production mainly involves a complex chemical synthesis route, which includes multiple reactions and the construction of specific intermediates. For instance, methods such as copper-mediated O-arylation reaction or SNAr reaction are used to introduce key aromatic oxygen groups. The synthesis process is continuously optimized towards the use of cheaper raw materials, improvement of reaction selectivity and yield. In terms of application, ABT-199 is widely used in cancer research, especially in studies related to the mechanism of cell apoptosis, and is often employed to explore pathological models of hematological diseases and potential treatment strategies.

Why can ABT-199 be used in cancer-related research?

After completing their tasks, human cells will naturally eliminate themselves through a "programmed cell death" mechanism, much like cells having their own "self-destruct mechanism". And the Bcl-2 protein is the "brake" of this self-destruct mechanism - it prevents cell apoptosis and keeps cells that should not continue to survive from leaving. In some studies on blood-related diseases, it was found that the Bcl-2 protein in cancer cells was abnormally increased, equivalent to the brake being pressed too hard, and the cells "couldn't die". Venetoclax Powder works like releasing this brake - it can selectively bind to the Bcl-2 protein, allowing the inhibited apoptotic pathway to restart and prompting abnormal cells to follow the normal process towards death. Due to this mechanism, ABT-199 has received extensive attention in the exploration of cell apoptosis regulation and the mechanism of blood system diseases.

What are the advantages of Venetoclax in experimental research?

The early attempts targeting the Bcl-2 target faced a challenging issue: although some compounds could block Bcl-2, they would also inhibit another protein called Bcl-XL, resulting in unwanted side effects - such as affecting the normal function of platelets. The advantage of Venetoclax Powder lies in its high selectivity for Bcl-2, enabling it to act more precisely on the target. Additionally, compared to other types of targeted molecules, the mutation rate of the Bcl-2 protein itself is relatively low, meaning that efficacy loss due to target mutations is less likely to occur in the experimental system. In actual research, scientists also combine ABT-199 with other research tools to explore the possibility of synergistic effects, for example, some studies have combined it with CAR-T cell therapy for experimental exploration in acute myeloid leukemia.

MF of ABT-199

CAS	1257044-40-8
Molecular formula	C45H50ClN7O7S
Molecular weight	868.44
EINECS	820-130-9
Melting point	>150°C
Density	1.340±0.06 g/cm3

Specification

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FAQ: 

Q1:Does ABT-199 act on any other targets besides Bcl-2?
It shows good selectivity at the commonly used concentrations. At higher concentrations, it may have certain effects on Bcl-XL or Bcl-w, but within the experimental concentration range, Bcl-2 is the main component.
Q2:How is the expression level of Bcl-2 protein in cells detected?

Commonly, immunoblotting or flow cytometry is used. Before the experiment, the expression level of Bcl-2 in the cell line can be detected to roughly predict the sensitivity to Venetoclax.

Q3:How was it verified in the experiment that ABT-199 actually binds to Bcl-2?

The binding affinity of the two can be determined by using fluorescence polarization competitive binding experiments or isothermal titration calorimetry.

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