ABT 263
- CAS No.
- 923564-51-6
- Chemical Name:
- ABT 263
- Synonyms
- Navitoclax;Navitoclax (ABT-263);ABT 263;CS-1871;CS-1967;Navitoclax-D8;ABT263;ABT-263;Navitoclax, >=98%;ABT 263 USP/EP/BP;ABT-263,Navitoclax
- CBNumber:
- CB21872884
- Molecular Formula:
- C47H55ClF3N5O6S3
- Molecular Weight:
- 974.61
- MDL Number:
- MFCD12756219
- MOL File:
- 923564-51-6.mol
Melting point | 114-116°C |
---|---|
Density | 1.41±0.1 g/cm3(Predicted) |
storage temp. | -20°C Freezer, Under Inert Atmosphere |
solubility | Soluble in DMSO (up to 25 mg/ml). |
pka | 4.60±0.10(Predicted) |
form | solid |
color | White |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
CAS DataBase Reference | 923564-51-6 |
NCI Dictionary of Cancer Terms | ABT-263; navitoclax |
FDA UNII | XKJ5VVK2WD |
NCI Drug Dictionary | navitoclax |
ABT 263 price More Price(32)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 11500 | ABT-263 ≥98% | 923564-51-6 | 1mg | $26 | 2024-03-01 | Buy |
Cayman Chemical | 11500 | ABT-263 ≥98% | 923564-51-6 | 5mg | $59 | 2024-03-01 | Buy |
Cayman Chemical | 11500 | ABT-263 ≥98% | 923564-51-6 | 10mg | $104 | 2024-03-01 | Buy |
Cayman Chemical | 11500 | ABT-263 ≥98% | 923564-51-6 | 25mg | $195 | 2024-03-01 | Buy |
TRC | A112500 | ABT263 | 923564-51-6 | 50mg | $215 | 2021-12-16 | Buy |
ABT 263 Chemical Properties,Uses,Production
Description
ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.
In vitro
ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. [1] ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263.
Description
ABT-263 (923564-51-6) is a potent and selective Bcl-2 family inhibitor / BH3 domain mimetic which binds to Bcl-2, Bcl-xL?and Bcl-w (Ki<1 nM). A useful tool compound which has shown interesting results in various cancer clinical trials.2?Synergizes with deoxyglucose and other agents, inducing apoptosis in cancer cells in a xenograft mouse model.3?A novel senolytic agent, inducing apoptosis preferentially in senescent cells in a cell type-restricted manner.4
Chemical Properties
Pale Yellow Solid
Uses
A novel inhibitor of antiapoptotic BCL-2 proteins; a new promising anticancer drug candidate.
Uses
ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.
Definition
ChEBI: Navitoclax is a N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of 4-{4-[(4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro[biphenyl]-2-yl)methyl]piperazin-1-yl}benzoic acid with the amino group of 4-{[(2R)-4-(morpholin-4-yl)-1-(phenylsulfanyl)butan-2-yl]amino}-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide. It is a BH3-mimetic drug which targets the anti-apoptotic B-cell lymphoma-2 (BCL-2) family proteins, including BCL-2, BCL-xL, and BCL-w, and induces apoptosis in cancer cells. Currently under clinical investigation as treatment for solid tumors and hematologic malignancies. It has a role as a B-cell lymphoma 2 inhibitor, an apoptosis inducer and an antineoplastic agent. It is a member of piperazines, a member of monochlorobenzenes, a member of morpholines, an aryl sulfide, a N-sulfonylcarboxamide, a sulfone, an organofluorine compound, a secondary amino compound and a tertiary amino compound.
Mechanism of action
ABT‐263 exerts its senolytic activity in senescent tumor cells by inhibiting BCL‐XL's interaction with BAX. ABT‐263 is a BH3 mimetic that inhibits anti‐apoptotic BCL‐2 family proteins by impeding their ability to bind pro‐apoptotic proteins, such as BAK and BAX. BCL‐2 and BCL‐XL are the primary targets of ABT‐263 in cancer cells.
storage
Store at -20°C
References
1) Tse?et al.?(2008),?ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor; Cancer Res.,?68?3421 2) Vogler?et al.?(2009),?Bcl-2 inhibitors: small molecules with a big impact on cancer therapy; Cell Death Differ.,?16?360 3) Yamaguchi?et al.?(2011),?Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy; PLoS ONE,?6(9)?e24102 4) Zhu?et al.?(2016),?Identification of a novel senolytic agent, navitoclax, targeting the Bcl-2 family of anti-apoptotic factors; Aging Cell,?15?428
ABT 263 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32820 | 60 |
Capot Chemical Co.,Ltd. | +86-(0)57185586718 +86-13336195806 | sales@capot.com | China | 29791 | 60 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21638 | 55 |
Hangzhou FandaChem Co.,Ltd. | +8615858145714 | FandaChem@Gmail.com | China | 9220 | 55 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29885 | 58 |
TianYuan Pharmaceutical CO.,LTD | +86-755-23284190 13684996853 | sales@tianpharm.com | CHINA | 304 | 58 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 965 | 58 |
Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 8497 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22963 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
Related articles
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- ABT 263 is a potent and orally bioavailable inhibitor of Bcl-2 family proteins, showing promise in treating hematological and ....
- Dec 6,2023
- ABT-263
- Navitoclax, also known as ABT-263 and ABT 263, is a potent, oral biologically active inhibitor of the Bcl-2 protein family, ac....
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View Lastest Price from ABT 263 manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-11-05 | Navitoclax
923564-51-6
|
US $41.00-88.00 / mg | 99.67% | 10g | TargetMol Chemicals Inc. | |||
2019-07-06 | ABT 263
923564-51-6
|
US $2.00 / KG | 1KG | 99% | customise | Career Henan Chemical Co |
- Navitoclax
923564-51-6
- US $41.00-88.00 / mg
- 99.67%
- TargetMol Chemicals Inc.
- ABT 263
923564-51-6
- US $2.00 / KG
- 99%
- Career Henan Chemical Co