ABT-263 (Navitoclax)
Catalog No. A10022
ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263 maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.
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| Catalog Num | A10022 |
|---|---|
| M. Wt | 974.6 |
| Formula | C47H55ClF3N5O6S3 |
| Purity | >98% |
| Storage | at -20°C 3 years Powder |
| CAS No. | 923564-51-6 |
| Synonyms | ABT263 |
| SMILES | CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)N[[email protected]](CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C |
ABT-263 also called Navitoclax is a potent and orally bioavailable Bcl-2 family inhibitor (Ki's of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w).ABT-263 maintains a high affinity for Bcl-xL, Bcl-2, and Bcl-w, (Ki ≤1 nmol/L), but binds more weakly to Mcl-1 and A1.
Targets
| Bcl-xL (Cell-free assay)[1] | Bcl-2 (Cell-free assay) | Bcl-w (Cell-free assay) | A1 (Cell-free assay) | Mcl-1 (Cell-free assay) |
| <=0.5 nM(Ki) | <=1 nM(Ki) | <=1 nM(Ki) | 354 nM(Ki) | 550 nM(Ki) |
In Vivo Studies
- Navitoclax was formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG (a dispersion of 50% phosphatidylcholine in a propylene glycol/ethanol carrier) and administered orally by gavage. [2]
- ABT-263 was formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG. [3]
- ABT-263 was administered orally at a dose of 100 mg/kg, daily for 21 days, as previously described . ABT-263 was also administered in combination with the conventional chemotherapeutic drugs vincristine (1 mg/kg, days 0 and 7), dexamethasone (15 mg/kg, Mon–Fri × 2 weeks) or l-asparaginase (1,500 U/kg, Mon-Fri × 2 weeks) on a Mon to Fri × 2-week schedule at least 1 hour after administration of the established drug. It was necessary to attenuate the dose of ABT-263 to 25 mg/kg when combined with vincristine, and to 50 mg/kg when combined with dexamethasone and l-asparaginase in order to achieve a tolerable dose. [4]
| In vitro | DMSO | 100 mg/mL (102.6 mM) | |
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 10.26 mL | 51.3 mL | 102.61 mL |
| 0.5 mM | 2.05 mL | 10.26 mL | 20.52 mL |
| 1 mM | 1.03 mL | 5.13 mL | 10.26 mL |
| 5 mM | 0.21 mL | 1.03 mL | 2.05 mL |
*The above data is based on the productmolecular weight 974.6. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
- Tse C, et al. ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836.
- Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9. doi: 10.1158/1535-7163.MCT-11-0415. Epub 2011 Sep 13.
- Shoemaker AR, et al. (2008) Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res 14(11):3268–3277.
- Santi Suryani, et al. Cell and molecular determinants of in vivo efficacy of the BH3 mimetic ABT-263 against pediatric acute lymphoblastic leukemia xenografts. Clin Cancer Res. 2014 Sep 1;20(17):4520-31. doi: 10.1158/1078-0432.CCR-14-0259. Epub 2014 Jul 10.
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