MedKoo Cat#: 202222
Name: Crizotinib
CAS#: 877399-52-5
Chemical Formula: C21H22Cl2FN5O
Exact Mass: 449.11854
Molecular Weight: 450.34
Elemental Analysis: C, 56.01; H, 4.92; Cl, 15.74; F, 4.22; N, 15.55; O, 3.55
Synonym: PF02341066; PF-02341066; PF 02341066; PF2341066; PF-2341066; PF 2341066; Crizotinib; US brand name: Xalkori;
IUPAC/Chemical Name: (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
InChi Key: KTEIFNKAUNYNJU-GFCCVEGCSA-N
InChi Code: InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
SMILES Code: NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1O[C@@H](C4=C(Cl)C=CC(F)=C4Cl)C
Technical Data
View CoA: current batch, Lot# TZC60627
View QC data: current batch, Lot# TZC60627
Additional Information
1. Crizotinib's phyisical and chemical properties:
Crizotinib is a white to pale-yellow powder with a pKa of 9.4 (piperidinium cation) and 5.6 (pyridinium cation).
2 . The solubility of crizotinib:
The solubility of crizotinib in aqueous media decreases over the range pH 1.6 to pH 8.2 from greater than 10 mg/mL to less than 0.1 mg/mL. The log of the distribution coefficient (octanol/water) at pH 7.4 is 1.65.
3. Mechanism of action:
Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON). Crizotinib has an aminopyridine structure, and functions as a protein kinase inhibitor by competitive binding within the ATP-binding pocket of target kinases . Crizotinib demonstrated concentration-dependent inhibition of ALK and c-Met phosphorylation in cell-based assays using tumor cell lines and demonstrated antitumor activity in mice bearing tumor xenografts that expressed EML4- or NPM-ALK fusion proteins or c-Met.
Crizotinib also inhibits the c-Met/Hepatocyte growth factor receptor (HGFR) tyrosine kinase, which is involved in the oncogenesis of a number of other histological forms of malignant neoplasms. Crizotinib is currently thought to exert its effects through modulation of the growth, migration, and invasion of malignant cells. Other studies suggest that crizotinib may also act via inhibition of angiogenesis in malignant tumors.(source: http://en.wikipedia.org/wiki/Crizotinib).
On August 26, 2011, the U.S. Food and Drug Administration approved crizotinib (Xalkori) to treat certain late-stage (locally advanced or metastatic) non-small cell lung cancers that express the abnormal anaplastic lymphoma kinase (ALK) gene.
References
1: Ou SH, Tong WP, Azada M, Siwak-Tapp C, Dy J, Stiber JA. Heart rate decrease during crizotinib treatment and potential correlation to clinical response. Cancer. 2013 Mar 15. doi: 10.1002/cncr.28040. [Epub ahead of print] PubMed PMID: 23505007.
2: Kaneda H, Okamoto I, Nakagawa K. Rapid Response of Brain Metastasis to Crizotinib in a Patient with ALK Rearrangement-Positive Non-Small-Cell Lung Cancer. J Thorac Oncol. 2013 Apr;8(4):e32-3. doi: 10.1097/JTO.0b013e3182843771. PubMed PMID: 23486271.
3: Maillet D, Martel-Lafay I, Arpin D, Pérol M. Ineffectiveness of Crizotinib on Brain Metastases in Two Cases of Lung Adenocarcinoma with EML4-ALK Rearrangement. J Thorac Oncol. 2013 Apr;8(4):e30-1. doi: 10.1097/JTO.0b013e318288dc2d. PubMed PMID: 23486270.
4: Pilotto S, Peretti U, Novello S, Rossi G, Milella M, Giaj Levra M, Ciuffreda L, Massari F, Brunelli M, Tortora G, Bria E. PROFILing non-small-cell lung cancer patients for treatment with crizotinib according to anaplastic lymphoma kinase abnormalities: translating science into medicine. Expert Opin Pharmacother. 2013 Apr;14(5):597-608. doi: 10.1517/14656566.2013.778828. Epub 2013 Mar 9. PubMed PMID: 23472711.
5: Sun Y, Nowak KA, Zaorsky NG, Winchester CL, Dalal K, Giacalone NJ, Liu N, Werner-Wasik M, Wasik MA, Dicker AP, Lu B. ALK inhibitor PF02341066 (crizotinib) increases sensitivity to radiation in non-small cell lung cancer expressing EML4-ALK. Mol Cancer Ther. 2013 Feb 26. [Epub ahead of print] PubMed PMID: 23443800.
6: Huang D, Kim DW, Kotsakis A, Deng S, Lira P, Ho SN, Lee NV, Vizcarra P, Cao JQ, Christensen JG, Kim TM, Sun JM, Ahn JS, Ahn MJ, Park K, Mao M. Multiplexed deep sequencing analysis of ALK kinase domain identifies resistance mutations in relapsed patients following crizotinib treatment. Genomics. 2013 Feb 20. doi:pii: S0888-7543(13)00034-7. 10.1016/j.ygeno.2013.02.006. [Epub ahead of print] PubMed PMID: 23434628.
7: Zheng X, He K, Zhang L, Yu J. Crizotinib induces PUMA-dependent apoptosis in colon cancer cells. Mol Cancer Ther. 2013 Feb 20. [Epub ahead of print] PubMed PMID: 23427294.
8: Srivastava N, VanderLaan PA, Kelly CP, Costa DB. Esophagitis: a novel adverse event of crizotinib in a patient with ALK-positive non-small-cell lung cancer. J Thorac Oncol. 2013 Mar;8(3):e23-4. doi: 10.1097/JTO.0b013e31827e2451. PubMed PMID: 23407563.
9: Browning ET, Weickhardt AJ, Camidge DR. Response to crizotinib rechallenge after initial progression and intervening chemotherapy in ALK lung cancer. J Thorac Oncol. 2013 Mar;8(3):e21. doi: 10.1097/JTO.0b013e31827a892c. PubMed PMID: 23407562.
10: Nonaka S, Yamaguchi S, Nagasawa T, Tahara M. [Pharmacology profile of crizotinib (Xalkori(®)Capsules) and clinical findings on this drug]. Nihon Yakurigaku Zasshi. 2013 Feb;141(2):106-13. Japanese. PubMed PMID: 23391552.
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(ResearchTrianglePark,简称RTP),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中 文美帝药库医药科技公司创立于2008年总部位于美国东海岸
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造,销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业,医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derivedRNA)与tracrRNA(trans-activatingRNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
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2.NaHCO3,Ba(OH)3,H2SO4
3.HCL,NaAlO2,NaHSO4
4.Ca(OH)2,Na2CO3,BaCO3
谢谢了
要原因
请问有什么方法检测细胞内活性氧更好,各位有什么经验,及相关试剂盒推荐一下。
A.H2SO4Na2SO4AgNO3BaCl2.
B.NaOHNa2CO3NaHSO4MgCl2
C.CaCl2NaNO3MgSO4BaCl2
D.HNO3KOHKClK2CO3
请问下有无同学需要H37RA的?我是做EAE模型的,上个月购买了BDDifco公司的H37RA(货号),因为购买的时候只能整盒6支购买,但我们用不了那么多,所以想问问有无同学需要的,100mg/支,800元/支或用等价试剂交换。地址广州。有需要的请私信,谢谢!
(1)优级纯试剂 亦称保证试剂,为一级品,纯度高,杂质极少,主要用于精密分析和科学研究,常以GR表示。
(2)分析纯试剂 亦称分析试剂,为二级品,纯度略低于优级纯,杂质含量略高于优级纯,适用于重要分析和一般性研究工作,常以AR表示。
(3)化学纯试剂 为三级品,纯度较分析纯差,但高于实验试剂,适用于工厂、学校一般性的分析工作,常以CP表示。
(4)实验试剂 为四级品,纯度比化学纯差,但比工业品纯度高,主要用于一般化学实验,不能用于分析工作,常以 LR表示。
以上按试剂纯度的分类法已在我国通用。根据化学工业部颁布的“化学试剂包装及标志”的规定,化学试剂的不同等级分别用各种不同的颜色来标志,见表1。
表1 我国化学试剂的等级及标志
bhclna2so4nano3na2co3
chclnaohna2co3nacl
dba(oh)2nahco3alcl3nahso4