Navitoclax (ABT-263) - 10mM in DMSO , CAS No.923564-51-6

CAS: 923564-51-6 Cat. No.: N408031 Molecular Weight: 974.61

GRADE & PURITY 10mM in DMSO

Synonyms

4-​[4-​[[2-​(4-​chlorophenyl)​-​5,​5-​dimethyl-​1-​cyclohexen-​1-​yl]​methyl]​-​1-​piperazinyl]​-​N-​[[4-​[[(1R)​-​3-​(4-​morpholinyl)​-​1-​[(phenylthio)​methyl]​propyl]​amino]​-​3-​[(trifluoromethyl)​sulfonyl]​phenyl]​sulfonyl]​-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Navitoclax (ABT-263) is a potent inhibitor ofBcl-xL,Bcl-2andBcl-wwithKiof ≤ 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. 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.

In vivo

When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens.
Cell Data

cell lines：

Concentrations：0-1 μM

Incubation Time：48 hours

Powder Purity:≥98%

Specifications

Synonyms

4-​[4-​[[2-​(4-​chlorophenyl)​-​5, ​5-​dimethyl-​1-​cyclohexen-​1-​yl]​methyl]​-​1-​piperazinyl]​-​N-​[[4-​[[(1R)​-​3-​(4-​morpholinyl)​-​1-​[(phenylthio)​methyl]​propyl]​amino]​-​3-​[(trifluoromethyl)​sulfonyl]​phenyl]​sulfonyl]​-benzamide

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Product Properties

• ALogP: 9.6

Names and Identifiers

• Isomeric SMILES: CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)N[C@H](CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C
• Molecular Weight: 974.61
• Reaxy-Rn: 15630714
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15630714&ln=

Associated Targets(Human)

MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 (2 Activities)

Discover Target: MCL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2 Tclin Apoptosis regulator Bcl-2 (5 Activities)

Discover Target: BCL2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2L1 Tchem Bcl-2-like protein 1 (6 Activities)

Discover Target: BCL2L1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2L2 Tchem Bcl-2-like protein 2 (2 Activities)

Discover Target: BCL2L2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ASPH Tchem Aspartyl/asparaginyl beta-hydroxylase (1 Activities)

Discover Target: ASPH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 64 mg/mL (197.3 mM); Water: Insoluble; Ethanol: Insoluble

References

1. Yun Zhou, Ke Li, Fan Li, Shuang Han, Yang Wang, Xueping Li, Yonghua Zhan.  (2019)  Doxorubicin and ABT-199 Coencapsulated Nanocarriers for Targeted Delivery and Synergistic Treatment against Hepatocellular Carcinoma.  Journal of Nanomaterials,      [PMID:] [10.1155/2019/5274598]

2. Ming Zhang, Yamei Wang, Yao Dai, Yan Hu, Wanting Fu, Yuhao Zhao, Hanyu Ma, Di Zhang, Ying Chen, Yixuan Zhou, Lei Du, Jing Chang, Fang Liu, Shuyan Chen, Fei Wang, Dongdong Xiao, Zhen Li.  (2025)  Senolytic-Loaded Asymmetric Wound Dressing for Targeted Senescent Cell Clearance in Diabetic Wound Healing.  Materials Today Bio,      [PMID:41560809] [10.1016/j.mtbio.2025.102741]

3. Jing Zhang, Xinghua Li, Ping Wang, Xin Liu, Wuqi Guo, Jia Si, Qiang Huo, Ming Xu, Yang Liu, Yimin Niu.  (2026)  Disrupting the Senescence-Associated Secretory Phenotype–M1Macrophage Feedback Loop in Synovitis Using Dual Nano-Switches To Restore Joint Homeostasis.  ACS Nano,      [PMID:41636104] [10.1021/acsnano.5c15543]