Venetoclax (ABT-199) - Moligand™, 10mM in DMSO , Apoptosis regulator Bcl-2 inhibitor, CAS No.1257044-40-8, Apoptosis regulator Bcl-2 inhibitor

CAS: 1257044-40-8 Cat. No.: V408685 Molecular Weight: 868.44 EC Number: 820-130-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

GDC-0199 | Benzamide, 4-[4-[[2-(4-chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Venetoclax (ABT-199, GDC-0199) is aBcl-2-selective inhibitor withKiof <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression,apoptosis, cell cycle
In vitro

ABT-199 shows less sensitivity to Bcl-xL, Mcl-1 and Bcl-w with K_i of 48 nM, > 444 nM and 245 nM, respectively. ABT-199 potently inhibits FL5.12-Bcl-2 cells, RS4;11 cells with EC50 of 4 nM and 8 nM, while shows low activity against FL5.12-Bcl-xL cells with EC50 of 261 nM. ABT-199 induces a rapid apoptosis in RS4;11 cells with cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA. Quantitative immunoblotting reveals that sensitivity to ABT-199 correlated strongly with the expression of Bcl-2, including NHL, DLBCL, MCL, AML and ALL cell lines. ABT-199 also induces apoptosis in CLL with an average EC50 of 3.0 nM.

In vivo

ABT-199 (100 mg/kg) causes a maximal tumor growth inhibition of 95% and tumor growth delay of 152% in RS4;11 xenografts. ABT-199 also inhibits xenograft growth (DoHH2, Granta-519) as a single agent or in combination with SDX-105 and other agents.
Cell Data

cell lines：

Concentrations：~1 μM

Incubation Time：48 hours

Powder Purity:≥98%

Specifications

Synonyms

GDC-0199 | Benzamide, 4-[4-[[2-(4-chlorophenyl)-4, 4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2, 3-b]pyridin-5-yloxy)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression,

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.

Grade

Moligand™

Action Type

ANTAGONIST, INHIBITOR

Mechanism of action

Apoptosis regulator Bcl-2 inhibitor

Product Properties

• ALogP: 8.2

Names and Identifiers

• Isomeric SMILES: CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
• Molecular Weight: 868.44
• Reaxy-Rn: 20908256
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20908256&ln=

Associated Targets(Human)

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

Discover Target: MCL1

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

BCL2 Tclin Apoptosis regulator Bcl-2 (10 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 (10 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)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 65 mg/mL (201.01 mM); Ethanol: 32 mg/mL (98.96 mM); Water: Insoluble
• Refractive Index: 1.64

References

1. Fengying Shao, Jianyu Han, Zhaoyan Tian, Zhi Wang, Songqin Liu, Yafeng Wu.  (2023)  Synergistic ROS generation and directional overloading of endogenous calcium induce mitochondrial dysfunction in living cells.  BIOMATERIALS,      [PMID:37619266] [10.1016/j.biomaterials.2023.122284]

2. Chen Zhigang, Zhang Yi, Li Wenlu, Gao Chenyi, Huang Fengbo, Cheng Lu, Jin Menglei, Xu Xiaoming, Huang Jian.  (2023)  Single cell profiling of female breast fibroadenoma reveals distinct epithelial cell compositions and therapeutic targets.  Nature Communications,  14  (1): (1-12).  [PMID:37328469] [10.1038/s41467-023-39059-3]

3. 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]