ABT-263 (Navitoclax)

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Bcl-2 inhibitor

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Catalog No. A10022

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
ABT-263 5mg A10022-5
$50.00
ABT-263 10mg A10022-10
$70.00
ABT-263 25mg A10022-25
$140.00
ABT-263 100mg A10022-100
$350.00
ABT-263 (Navitoclax) 10mM * 1mL in DMSO A10022-10mM-D
$156.00

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

ABT-263 (Navitoclax) is a potent orally bioavailable SMI that is structurally related to ABT-737. ABT-263 disrupts Bcl-2 - Bcl-XL interactions with pro-apoptotic proteins .

ABT-263 (Navitoclax)

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Chemical Information

Catalog Num A10022
Actions Inhibitor
M. Wt 974.6
Formula C47H55ClF3N5O6S3
Solubility DMSO
Purity >98%
Storage at -20°C 2 years
CAS No. 923564-51-6
Synonyms ABT263
SMILES code 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
Chemical Name (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide

Biological Activity

Description
ABT-263 (Navitoclax) is a potent orally bioavailable SMI that is structurally related to ABT-737. ABT-263 disrupts Bcl-2 - Bcl-XL interactions with pro-apoptotic proteins .
Targets
Bcl-xL (Cell-free assay) 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)

Solubility

Solubility (25°C)* 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.

Biological Activity

Phase I study of Navitoclax (ABT-263):

Forty-seven patients, including 29 with small-cell lung cancer (SCLC) or pulmonary carcinoid, were enrolled between 2007 and 2008, 35 on intermittent and 12 on continuous dosing cohorts. Primary toxicities included diarrhea (40%), nausea (34%), vomiting (36%), and fatigue (34%); most were grade 1 or 2. Dose- and schedule-dependent thrombocytopenia was seen in all patients. One patient with SCLC had a confirmed partial response lasting longer than 2 years, and eight patients with SCLC or carcinoid had stable disease (one remained on study for 13 months). Pro-gastrin releasing peptide (pro-GRP) was identified as a surrogate marker of Bcl-2 amplification and changes correlated with changes in tumor volume. CONCLUSION:  Navitoclax is safe and well tolerated, with dose-dependent thrombocytopenia as the major adverse effect. Preliminary efficacy data are encouraging in SCLC. Efficacy in SCLC and the utility of pro-GRP as a marker of treatment response will be further evaluated in phase II studies.

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General References

1. Methods and means for the treatment of cancer using a combination of a BCRP inhibitor and/or a P-gp inhibitor with an imidazotetrazine chemotherapeutic agent By Van Tellingen, Olaf From U.S. Pat. Appl. Publ. (2009), US 20090170880 A1 20090702.
2. Quinazolin-4-ylaminopyrazolecarboxamides as aurora kinase inhibitors useful in bombination therapy for the treatment of cancer and their preparation By Keen, Nicholas John From PCT Int. Appl. (2007), WO 2007132215 A1 20071122.
3. Structure-activity relationships of a series of tariquidar analogs as multidrug resistance modulators By Globisch, Christoph; Pajeva, Ilza K.; Wiese, Michael From Bioorganic & Medicinal Chemistry (2006), 14(5), 1588-1598.
4. Means and methods for treating a disease which is associated with an excess transport of hyaluronan across a lipid bilayer By Prehm, Peter From PCT Int. Appl. (2005), WO 2005013947 A2 20050217.
5. P glycoprotein in human immunodeficiency virus type 1 infection and therapy By Sankatsing, Sanjay U. C.; Beijnen, Jos H.; Schinkel, Alfred H.; Lange, Joep M. A.; Prins, Jan M. From Antimicrobial Agents and Chemotherapy (2004), 48(4), 1073-1081.

View Related Products By Research Topics

Cat. No.

Product NameSolubility(mg/mL)
WaterDMSOEthanol
A10255 ABT-737 <1 mg/mL 163 mg/mL <1 mg/mL
A10022 ABT-263 (Navitoclax) <1 mg/mL 195 mg/mL <1 mg/mL
A10665 Obatoclax mesylate (GX15-070) <1 mg/mL 83 mg/mL <1 mg/mL
A10955 TW-37 <1 mg/mL 115 mg/mL 4 mg/mL
A10984 VX-765 <1 mg/mL 102 mg/mL 102 mg/mL
A11090 PAC-1 <1 mg/mL 78 mg/mL 16 mg/mL
A10491 JNJ 26854165 <1 mg/mL 66 mg/mL 2 mg/mL
A11931 RITA (NSC 652287) <1 mg/mL 115 mg/mL 4 mg/mL
A10522 Lenalidomide (CC-5013) <1 mg/mL 52 mg/mL <1 mg/mL
A10743 Pomalidomide (CC-4047) <1 mg/mL 55 mg/mL <1 mg/mL
A11163 AT-406 <1 mg/mL 112 mg/mL 112 mg/mL
A11002 YM155 89 mg/mL 55 mg/mL 6 mg/mL
A10935 Tipifarnib (Zarnestra) <1 mg/mL 83 mg/mL <1 mg/mL
A10657 Nutlin-3 <1 mg/mL 116 mg/mL 116 mg/mL
A11635 Cyclophosphamide monohydrate 20 mg/mL 56 mg/mL <1 mg/mL

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