Idarubicin HCl
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.
Idarubicin是DNA拓扑异构酶II的抑制剂[1]。
Idarubicin是一种合成的蒽环类抗癌药,广泛应用于急性髓性白血病和一些其他恶性白血病的治疗。Idarubicin可被NADPH-细胞色素C还原酶活化,导致DNA单链断裂的形成。这就是Idarubicin的抗肿瘤机理[2]。
Idarubicin是在一次降低母体化合物的心脏毒性并提高其治疗效果的尝试中发现的。与其母体化合物不同,Idarubicin可口服,且相对其心脏毒性有更好的治疗指数。Idarubicin也是一种有效的适用于儿童和成人的抗白血病制剂[3]。
参考文献:
[1] H. Dorota Halicka, M. Fevzi Ozkaynak, Oya Levendoglu-Tugal, Claudio Sandoval , Karen Seiter, Malgorzata Kajstura, Frank Traganos, Somasunadaram Jayabose, and Zbigniew Darzynkiewicz. DNA damage response as a biomarker in treatment of leukemias. Cell Cycle. 2009, 8(11): 1720–1724.
[2] Haydar elik and Emel Arin. Evaluation of the Protective Effects of Quercetin, Rutin, Resveratrol, Naringenin and Trolox Against Idarubicin-Induced DNA Damage. J Pharm Pharmaceut Sci. 2010, 13(2): 231 – 241.
[3] Ching-Hon Pui, Siebold S. N. de Graaf, Lois W. Dow, John H. Rodman, William E. Evans, Bruce S. Alpert and Sharon B. Murphy. Phase I Clinical Trial of Orally Administered 4-Demethoxydaunorubicin (Idarubicin) with Pharmacokinetic and in Vitro Drug Sensitivity Testing in Children with Refractory Leukemia. Cancer Research. 1988, 48: 5348-5352.
Storage | Store at -20°C |
M.Wt | 533.95 |
Cas No. | 57852-57-0 |
Formula | C26H28ClNO9 |
Solubility | ≥26.7 mg/mL in DMSO; insoluble in EtOH; ≥2.39 mg/mL in H2O with ultrasonic |
Chemical Name | (7S,9S)-9-acetyl-7-(((2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-6,9,11-trihydroxy-7,8,9,10-tetrahydrotetracene-5,12-dione hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C(C1=C2C(O)=C3C([C@@H](O[C@]4([H])O[C@@H](C)[C@@H](O)[C@@H](N)C4)C[C@](O)(C(C)=O)C3)=C1O)C5=CC=CC=C5C2=O.Cl |
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 |
NALM-6细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
0.1 nM ~ 10 μM;24小时 |
实验结果 |
在NALM-6细胞中,Idarubicin抑制细胞增殖,其IC50值为12 nM。 |
动物实验 [2]: | |
动物模型 |
大鼠、兔、小鼠和狗 |
给药剂量 |
2 mg/kg,0 mg/kg ~ 75 mg/kg,3 mg/kg和0 mg/kg ~ 75 mg/kg;静脉注射 |
实验结果 |
还原取决于酮还原酶,具有比大多数酮更高的立体选择性。Idarubicin还原的高立体选择性可能是由于手性诱导(Idarubicin羰基附近存在不对称中心)导致的。 |
其他注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Rowland AJ, Pietersz GA, McKenzie IF. Preclinical investigation of the antitumour effects of anti-CD19-idarubicin immunoconjugates. Cancer Immunol Immunother. 1993 Aug;37(3):195-202. [2]. Strolin Benedetti M, Pianezzola E, Fraier D, Castelli MG, Dostert P. Stereoselectivity of idarubicin reduction in various animal species and humans. Xenobiotica. 1991 Apr;21(4):473-80. |
质量控制和MSDS
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