1257044-40-8
ABT-199
CAS: 1257044-40-8
Molecular Formula: C45H50ClN7O7S
1257044-40-8 - Names and Identifiers
1257044-40-8 - Physico-chemical Properties
| Molecular Formula | C45H50ClN7O7S |
| Molar Mass | 868.44 |
| Density | 1.340±0.06 g/cm3(Predicted) |
| Melting Point | >150°C (dec.) |
| Appearance | Form Yellow solid, color Light Yellow to Yellow |
| pKa | 4.09±0.10(Predicted) |
| Storage Condition | -20°C Freezer |
| Physical and Chemical Properties | Bioactive ABT-199 (GDC-0199) is a Bcl-2 selective inhibitor. Ki is <0.01 nM in cell-free test, which is more than 4800 times higher than the selectivity of acting on Bcl-xL and Bcl-w, and has no inhibitory activity on Mcl-1. |
1257044-40-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.151 ml | 5.757 ml | 11.515 ml |
| 5 mM | 0.23 ml | 1.151 ml | 2.303 ml |
| 10 mM | 0.115 ml | 0.576 ml | 1.151 ml |
| 5 mM | 0.023 ml | 0.115 ml | 0.23 ml |
Last Update：2024-01-02 23:10:35
1257044-40-8 - Uses and synthesis methods
novel anticancer drugs
ABT-199 is a new type of anti-cancer drug. It is a Bcl-2 inhibitor. It is developed by the American pharmaceutical company AbbVie. It can effectively resist cancer and will produce compared with current drugs. Less side effects, this research is mainly completed by researchers in the United States and Australia, and the relevant research results are published in the International Journal Nature Medicine.
Different from ordinary cancer drugs, this drug named ABT-199 treats cancer by attacking an important protein called BCL-2. BCL-2 is one of the earliest discovered members of the cell death regulatory BCL-2 protein family. It is associated with many types of cancer, as well as some mental and autoimmune diseases. In cancer, it is thought to act as a suppressor that can help cancer cells resist cancer treatment drugs.
In the treatment of cancer, cancer cells can use pro-survival protein BCL-2 to inhibit the therapeutic effect of traditional chemotherapy, which often makes clinicians headache. It is precisely because cancer cells can use pro-survival protein BCL-2 to inhibit the therapeutic effect of traditional chemotherapy, which makes clinical therapists have to increase the dose again and again, which leads to chemotherapy side effects such as nausea and alopecia.
the emergence of ABT-199 as a drug that can eliminate and reduce BCL-2 in cancer cells has made many clinicians see the dawn of cancer treatment. As a new anticancer drug, ABT-199 can not only inhibit BCL-2 growth, but also not affect BCL-XL-a protein necessary for platelet formation. The overcoming of this problem is completely worthy of joy in the history of tumor treatment.
[clinical trial evaluation]: phase I clinical trial (NCT01328626) enrolled 84 patients with recurrent/refractory CLL/SLL and 44 patients with recurrent/refractory non-Hodgkin lymphoma. The response rate of CLL/SLL ABT-199 treatment was 79% (complete response rate was 22%), and the median sustained response time was 20.5 months. The response rate for ABT-199 treatment of non-Hodgkin lymphoma was 48% (complete response rate was 7.5%). The efficacy of ABT-199 can match that of obinutuzumab, idelalisib and ibrutinib, and is expected to become the first Bcl-2 inhibitor on the market.
in vitro studies
ABT-199 have low sensitivity to Bcl-xL, Mcl-1 and Bcl-w, Ki is 48 nM, >444 nM and 245 nM respectively. ABT-199 effectively inhibited FL5.12-Bcl-2 cells, RS4;11 cells, EC50 is 4 nM and 8 nM respectively, have low activity on FL5.12-Bcl-xL cells, EC50 is 261 nM. ABT-199 induces RS4; Rapid apoptosis, cytochrome c release, caspase activation, phosphatidylserine externalization, and sub-G0/G1 DNA accumulation in 11 cells. Quantitative immunoblotting showed that the sensitivity of ABT-199 to cell lines including NHL,DLBCL,MCL,AML and ALL was strongly correlated with the expression of Bcl-2. ABT-199 also induced CLL apoptosis with an average EC50 of 3.0 nM.
In vivo studies
ABT-199 (100 mg/kg) treated RS4;11 transplanted tumors, the maximum tumor growth inhibition rate was 95%, and the tumor growth delay was 152%. ABT-199 treatment of DoHH2 and Granta-519 transplanted tumors alone or in combination with SDX-105 and other agents also inhibits tumor growth.
features
Reorganization of ABT-263 (Navitoclax).
Last Update：2024-04-10 22:29:15
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Product Name: Venetoclax Visit Supplier Webpage Request for quotationCAS: 1257044-40-8
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: ABT-199 Venetoclax Visit Supplier Webpage Request for quotationCAS: 1257044-40-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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