Purvalanol B
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Purvalanol B 是一种选择性的CDK1、CDK2 和CDK4抑制剂。
CDKs (细胞周期蛋白依赖性激酶)家族可以调节细胞周期。
据报道,Purvalanol B是最强效的和选择性的CDK 抑制剂之一。在中国仓鼠肺成纤维CCL39细胞系中,Purvalanol B通过靶向CKD1,诱导G2/M 期阻滞,抑制细胞增殖,GI50为2.5 μM。在异步细胞中,接受Purvalanol B治疗导致G2/M期细胞的积累。
在NCI-H2228 皮下异种移植的小鼠模型中,口服给药ASP3026引起磷酰化ALK和肿瘤生长的显著减少。持续两周给药ASP3026 30 mg/kg/d导致78%的肿瘤消退。在注射Karpas 299 细胞的小鼠中,ASP3026 治疗引起显著的淋巴瘤消退[ 2 ,3 ] 。
在包括MCF-7细胞系在内的几个哺乳动物细胞系中,Purvalanol B 也与p42/p44 MAPK 蛋白质相互作用 [ 1 ] 。
参考文献:
1.Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026, a novel and selective ALK inhibitor of anaplastic lymphoma kinase (ALK). Annual Meeting of the American Association for Cancer Research (AACR), Orlando, FL. 2011.
2.Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340.
3.George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763
.Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 432.9 |
Cas No. | 212844-54-7 |
Formula | C20H25ClN6O3 |
Synonyms | NG 95; NG95; NG-95 |
Solubility | ≥21.65 mg/mL in DMSO; insoluble in H2O; ≥2.57 mg/mL in EtOH with gentle warming |
Chemical Name | 2-chloro-4-[[2-[[(2R)-1-hydroxy-3-methylbutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]benzoic acid |
SDF | Download SDF |
Canonical SMILES | CC(C)C(CO)NC1=NC2=C(C(=N1)NC3=CC(=C(C=C3)C(=O)O)Cl)N=CN2C(C)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
中国仓鼠肺成纤维细胞CCL39细胞系,异步细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于21.7 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
2.5 μM |
应用 |
在中国仓鼠肺成纤维细胞CCL39细胞系中,Purvalanol B通过靶向CKD1抑制细胞增殖,其阻断G2/M的GI50为2.5 μM。在异步细胞中,Purvalanol B导致G2/M期细胞的积累。 |
动物实验 [2, 3]: | |
动物模型 |
皮下异种移植NCI-H2228和Karpas 299细胞的小鼠模型 |
给药剂量 |
口服,30 mg/kg/d,2周 |
应用 |
在NCI-H2228皮下异种移植的小鼠模型中,口服ASP3026显著降低磷酸化ALK和肿瘤生长。ASP3026 (30 mg/kg/d, 2周)诱导78%肿瘤消退。在注射Karpas 299细胞的小鼠中,ASP3026治疗引起显著的淋巴瘤消退。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026,–A novel and selective ALK inhibitor[J]. 2011. [2]. Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340. [3].George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763. |
质量控制和MSDS
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