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My CartCAS：866541-93-7
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light brown to black Solid
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| CAS | 866541-93-7 |
| Name | (R)-(-)-Gossypol Acetic Acid |
| Molecular Formula | C32H34O10 |
| Molecular Weight | 578.61 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light brown to black Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| SMILES | OC1=C2C(C=O)=C(O)C(O)=C(C(C)C)C2=CC(C)=[C@]1[C@]3=C(C)C=C4C(C(C)C)=C(O)C(O)=C(C=O)C4=C3O.CC(O)=O.[R] |
| Target Point | Bcl-2 Family;Bcl-xL;Mcl-1 |
| Passage | Apoptosis |
| Background | It is a potent inhibitor of Bcl-2,Bcl-xL and Mcl-1. |
| Biological Activity | (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) 是天然产物 Gossypol 的左旋异构体。AT-101 结合到 Bcl-2，Mcl-1 和 Bcl-xL 蛋白，Ki 值分别为 260±30 nM，170±10 nM 和 480±40 nM。[1-2] |
| In Vitro | (R)-(-)- 棉酚(AT-101)和(+)- 棉酚与具有相似结合亲和力的Bcl-2或Bcl-xL结合，AT-101比(+)- 棉酚抑制细胞更有效。生长和诱导细胞凋亡，可能是由于血清在细胞培养实验中的影响。在6天MTT测定中，针对UM-SCC-6和UM-SCC-14A测试外消旋形式和棉酚的每种对映体。(R)-(-)- 棉酚(AT-101)在所测试的两种细胞系中相对于(±)- 棉酚表现出比(+)- 棉酚更大的生长抑制(P <0.001)。用(±)- 棉酚观察到中间生长抑制作用，但这种作用仅在较高剂量的棉酚(10μM，P <0.0001)下观察到。(R)-(-)- 棉酚(AT-101)以相当高的亲和力结合Bcl-xL和Bcl-2蛋白的BH3结合沟，对头颈部鳞状细胞癌(HNSCC)细胞系具有强大的活性。体外。此外，它在表达功能性p53的HNSCC肿瘤细胞中高效诱导细胞凋亡，并且还通过不同的机制杀死具有突变体p53的肿瘤细胞。(R)-(-)- 抑制人成纤维细胞系生长50％所需的棉酚(AT-101)剂量比HNSCC细胞系高2至10倍。为了抑制人口腔角质形成细胞生长50％，(R)-(-)- 棉酚(AT-101)浓度比HNSCC细胞系高2至3倍。(R)-(-)- 棉酚(AT-101)在6天MTT测定中引起10种UM-SCC细胞系中细胞生长的剂量依赖性抑制，范围为0.5至10μM。细胞系的相对敏感性不同于IC50为2-5μM的非常敏感组和IC50聚集在10μM左右的敏感性较低的组[1]。(R)-(-)- 棉酚(AT-101)被确定与Bcl-2，Mcl-1和Bcl-xL蛋白结合，Ki值为260±30 nM，170±10 nM和480±40 nM分别为[2]。 |
| Cell Experiment | 两种代表性的UM-SCC细胞系UM-SCC-6和UM-SCC-14A持续暴露于0(载体对照)，5或10μM(±)- 棉酚，(R)-(-)- 棉酚(AT-101)或(+)- 在6天MTT细胞存活试验中的棉酚[1]。 |
| Data Literature Source | [1]. Oliver CL，et al. In vitro effects of the BH3 mimetic，(-)-Gossypol，on head and neck squamous cell carcinoma cells. Clin Cancer Res. 2004 Nov 15;10(22):7757-63. [2]. Sun Y，et al. Apogossypolone，a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins，effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo. Cancer Biol Ther. 2008 Sep;7(9):1418-26. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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