A-1155463 纯度:98.55% 200mg

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A-1155463 纯度:98.55% 200mg

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货号：HY-19725

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商品介绍
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A-1155463是高效选择性的BCL-X_L抑制剂，在Molt-4细胞中的EC₅₀值为70 nM。

Description

A-1155463 is a highly potent and selective BCL-X_L inhibitor with a EC₅₀ value of 70 nM in Molt-4 cell.

IC₅₀ & Target^[2]

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 EC₅₀ values ≤0.5 μM in the presence of 10 % FBS^[3].

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].

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (74.65 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

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 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (3.73 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: ≥ 2.5 mg/mL (3.73 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (3.73 mM); Clear solution

References

[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med.?2015 Mar 18;7(279):279

[2]. Tao ZF, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93.

[3]. Zhang H, et al. Genomic analysis and selective small molecule inhibition identifies BCL-X(L) as a critical survival factor in a subset of colorectal cancer. Mol Cancer. 2015 Jul 2;14:126.

Animal Administration ^[2]	Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-1155463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells with a daily dose at 5 mg/kg IP for 14 days^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Leverson JD, et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med.?2015 Mar 18;7(279):279 [2]. Tao ZF, et al. Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity. ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. [3]. Zhang H, et al. Genomic analysis and selective small molecule inhibition identifies BCL-X(L) as a critical survival factor in a subset of colorectal cancer. Mol Cancer. 2015 Jul 2;14:126.

Animal Administration
^[2]

Mice: Following a single 5 mg/kg IP dose of A-1155463 in nontumor bearing SCID-Beige mice, platelet counts fell dramatically as measured at 6 h postdose and then rebounded to normal levels within 72 h. A-1155463 is then administered to SCID-Beige mice that had been inoculated with BCL-XL-dependent H146 tumor cells with a daily dose at 5 mg/kg IP for 14 days^[2].

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

References