Top quality raw material Olaparib for Breast and ovarian cancer treatment CAS NO.763113 22 0

Product name: Olaparib
Appearance: white powder

CAS NO.:  763113-22-0

Molecular formula: C24H23FN4O3
Molecular weight: 434.469

Density: 1.43

Uses: 

Olaparib is a kind of novel poly ADP-ribose polymerase (PARP) inhibitors, including PARP1, PARP2, and PARP3. PARP mediates a DNA-repair mechanism which plays a important role in DNA damage repair and apoptosis, so olaparib specifically targets on the DNA repair mechanism of the targeting cell DNA repair and take effects by attacking the critical vulnerabilities of cancer cells carrying mutations in BRCA1 and BRCA2. Owing to this mechanism, it can be used for the maintenance therapy of patients of severe recurrent ovarian cancer who has breast cancer susceptibility gene (BRCA) mutation as well as being sensitive to platinum drug. Scientists from Harvard Medical School Dana-Farber Cancer Institute have found that the target site of olaparib is the polymerase Q (POLQ, also known POLθ). Those scientists found that a large number of patients of ovarian cancer has the genetic deficiency in the homologous recombination (homologous recombination, HR) repair pathway and dramatic up-regulated expression of POLQ greatly. Since HR is an important repair pathway for repairing broken DNA, they speculated that the major function of POLQ is to compensate for the lack of HR and participate in DNA repair. The experiment has demonstrated that, in normal HR cells, knockout of POLQ would make HR activity increase significantly; while in HR deficient cells, the knockout of POLQ leads to cell death. POLQ contains RAD51 binding domain which can block the process of RAD51-mediated DNA repair. Related research has been published in the February 12, 2015 Nature journal with Raphael Ceccaldi being the first author of this research. Studies have revealed that about 10% of ovarian cancer patients and 5% of breast cancer patients contain BRCA1 or BRCA2 mutations. Both BRCA1 and BRCA2 belong to tumor suppressor genes as the major components of HR repair pathway. Their mutation suggests the loss of function for the HR repair pathway. In the cancer model of BRCA1 or BRCA2 mutations, blocking the important component for repairing single-strand DNA breaks--PARP can kill the mutated cancer cells. Put the BRCA-deficient mice with POLQ deficient mice for hybridization will cause the death of mouse embryos shortly after birth, which means that the coexistence of two repair pathway deficiency will cause embryonic lethality. These above findings suggest that olaparib, a kind of novel oral PARP inhibitor which is able to kill BRCA deficient cells, may be the effective drug for treating cancer patients who carry such mutations. Previously, researcher s knowledge of the BRCA mutation hasn t influenced patients choice of treatment on either ovarian cancer or breast cancer. However, after the study, which means that olaparib can be used for the targeted therapy of cancer patients who carries BRCA1 or BRCA2 gene mutations with the therapeutic target site being the genetic deficiency of cancer cell genetic defect rather than a target organ. In ovarian and breast cancer cells, BRCA mutations are the first heavy blow to the survivability of cell because it increases their susceptibility to DNA damage. Through targeting the PARP-controlled adjuvant repair pathways, olaparib and its similar drugs achieve the second heavy blow to the survivability of cell. With the disorders of both of the two repairmen signaling pathways, the accumulation of DNA damage exert the third heavy blow to the cells.

Specifications:

Item	Specifications	Results
Appearance	White to  light yellow powder	Conforms
Loss on drying	≤0.2%	0.02%
Water content(KF)	≤0.5%	0.03%
Purity(by HPLC)	≥98.5%	98.90%
Heavy metal	≤20 ppm	Conforms
NMR Spectrum	Sample correspond to that of standard preparation	Conforms
Total impurities	≤0.5%	Conforms

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Company introduction.

Famouschem Technology(Shanghai) Co., Ltd. is established in 2012 and located in Shanghai---the economic center of China. We have one workshop with production capacity of 5000 tons per year, and one research and test center which is located in Jiangsu province. In Shanghai office, there still has a professional sales team whose average exporting experience is over 4 years.
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Famouschem has its own unique experimentatal plateform, and is constructing a standard CMC R&D center. Meanwhile,we have established close cooperation with GMP and FDA cGMP factories.Famouschem can provide you with products and technical support that meet the requirements of new drug research and development at all stages.

With excellent quality products and good service, our products have been widely used all around the world. 

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The QC department equipped with a lot of professional equipment,include Agilent  HPLC(with DAD&ELSD detectors),polarimeter,Melting Point meter,water analyzer,etc.

MS&NMR data can also be tested by our long-term partners.

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For large quantity products, shipment is better. It will cost days to weeks to come to your destination port, which depends on where the port is.

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