HENAN SUNLAKE ENTERPRISE CORPORATION
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Business Type:Trading Company
Tel: +86-371- 86259723
Tel: 17734809689
Tel: 17734809689
Tel: 86-371-86259723
Tel: 17734809689
Tel: 17734809689
Mobile: 17734809689
Tel: +86-371- 86259723
Fax: +86-371- 86259723
Province/state: HENAN
City: ZHENGZHOU
Street: Mingmen International Center, NO.222 Dongming Road,Zhengzhou,Henan,China
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HENAN SUNLAKE ENTERPRISE CORPORATION
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ABT-199 Basic information
| A new type of anti-cancer drugs Biological Activity In vitro studies In vivo studies Characteristics |
| Product Name: | ABT-199 |
| Synonyms: | ABT-199;ABT199,GDC0199;GDC 0199;GDC0199;GDC-0199;4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide;Benzamide, 4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-;4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-benzamide ABT-199 (GDC-0199) |
| CAS: | 1257044-40-8 |
| MF: | C45H50ClN7O7S |
| MW: | 868.4392 |
| EINECS: | -0 |
| Product Categories: | Apis;Inhibitor;Inhibitors |
| Mol File: | 1257044-40-8.mol |
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| ABT-199 Chemical Properties |
| Safety Information |
| ABT-199 Usage And Synthesis |
| A new type of anti-cancer drugs |
ABT-199 is a novel anti-cancer drug, and a Bcl-2 inhibitor, which is researched and developed by by the US pharmaceutical company Abbvie (AbbVie).It is effective against cancer, and makes a small side effects compared to the current drugs, The study is carried out by US and Australian researchers, and their research results were published in the international journal Nature Medicine. It is different from common cancer drugs: this drug named ABT-199 attacks one kind of important proteins referred as BCL-2 to play an important role in the treatment of cancer. BCL-2 is the first discovered member of cell death regulating BCL-2 protein family . It is associated with many types of cancer, as well as some psychiatric disorders and autoimmune diseases. In cancer, people think it acts as a repressor that can help cancer cells to resist cancer treatments. In the treatment of cancer, cancer cells can make use of pro-survival BCL-2 protein to inhibit the therapeutic effect of conventional chemotherapy, which often gives clinicians headache. It is also because the cancer cells can be make use of pro-survival BCL-2 protein to inhibit the therapeutic effect of conventional chemotherapy, that makes clinical doctors have to increase the dose again and again, which leads to the side effects of chemotherapy, such as nausea, hair loss and so on. ABT-199 emerging as a drug to eliminate and reduce the occurrence of BCL-2, makes many clinicians see the dawn of cancer treatment. ABT-199 as a novel anti-cancer drug, can inhibit the growth of BCL-2, without affecting BCL-XL-- a protein necessary for platelet formation . Overcoming this problem, is completely worth cheering in the history of the treatment of cancer. [Clinical Trial Evaluation] clinical trial phase I (NCT01328626) enrolls 84 patients with relapsed type / refractory CLL / SLL and 44 patients with relapsing / refractory non-Hodgkin's lymphoma . ABT-199 treatment of CLL / SLL response rate is 79% (complete response rate was 22%), median durative response time is 20.5 months; ABT-199 treatment of non-Hodgkin's lymphoma response rate is 48% (complete The response rate was 7.5%). The efficacy of ABT-199 is well matched with obinutuzumab, idelalisib, ibrutinib. ABT-199 is expected to be the first Bcl-2 inhibitor on the market. The above information is edited by the chemicalbook of Tian Ye. |
| Biological Activity | ABT-199 (GDC-0199) is a selective inhibitor of Bcl-2, Ki is <0.01 nM in a cell-free assay , selectivity in Bcl-2 is over 4800 times higher than that in Bcl-xL and Bcl-w ,it has no inhibitory activity in Mcl-1 . |
| In vitro studies | ABT-199 has a low sensitivity to Bcl-xL, Mcl-1 and Bcl-w , Ki is 48 nM,> 444 nM and 245 nM. ABT-199 effectively inhibits FL5.12-Bcl-2cells, RS4; 11 cells, EC50 is 4 nM and 8 nM, it has low activity on FL5.12-Bcl-xLcells , EC50 is 261 nM. ABT-199 induces RS4; 11 cells into apoptosis rapidly and releases cytochrome c , activates caspase , externalizes phosphatidylserine and accumulates sub-G0 / G1 DNA . Quantitative immunoblotting shows, ABT-199 sensitivity to cell lines including NHL, DLBCL, MCL, AML and ALL , is strongly related to Bcl-2 expression . ABT-199 also induces apoptosis of CLL, the mean EC50 is 3.0 nM. |
| In vivo studies | ABT-199 (100 mg / kg) treats RS4; 11 xenografts, maximum growth inhibition of the tumors is 95%, tumor growth delays 152%. ABT-199 alone or in combination with SDX-105 or other agents treating DoHH2 and Granta-519 xenografts, also inhibits tumor growth. |
| Characteristics | ABT-263 (Navitoclax) restructuring. |
Henan Sunlake Enterprise Corporation is located in Henan Province , The central plain of China , Which enjoys favorable geogeaphical position and convenient transportion. The com[any was established in june. 1998, until now having more than 18 years experience in manufacturing & exporting chemical raw material .
Sunlake is a professional manufacturer engaged in producing and selling chemicals,including Organic & inorganic chemicals , pigments & Dyestuffs , Water treatment chemicals , Food & FEED additives and others. These products have been being well exported to europe, southeast Asia, the Middle East ,Africa, South America and some other countries and areas.
We sincerely welcome foreign friends to visit our plant for cooperation. With the idea of "quality first,credit priority, Excellent service", We are highly acknowledged by customers for good quality and competitive price. More importantly , the company has a strong R & D team, who are professional engineers and scholars with Ph. D. .So we are confident to serve you better with our high - quality products and professional team. We are taking great efforts to provide our customers with demanded goods and professional services, and continuously improve our core ability of competition and get the momentum for sustainable development, and finally make us being a reliable and professional supplier in international market.
We welcome any serious inquiries from all customers of the world, and sincerely hope to cooperate with you for a brilliant future!
