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

  • 10mM in DMSO
Item Number
N408031
Grouped product items
SKUSizeAvailabilityPrice Qty
N408031-1ml
1ml
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$47.90

Bcl-2 Selective Inhibitors | Antagonists | Modulators

Basic Description

Specifications & Purity10mM in DMSO
Biochemical and Physiological MechanismsNavitoclax (ABT-263) 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.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
Product Description

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%

Product Properties

Ki DataBcl-2, Ki: <=1 nM

Associated Targets(Human)

MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCL2 Tclin Apoptosis regulator Bcl-2 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCL2L1 Tchem Bcl-2-like protein 1 (6 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCL2L2 Tchem Bcl-2-like protein 2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ASPH Tchem Aspartyl/asparaginyl beta-hydroxylase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

Canonical SMILES CC1(C)CCC(=C(CN2CCN(CC2)C3=CC=C(C=C3)C(=O)N[S](=O)(=O)C4=CC(=C(NC(CCN5CCOCC5)CSC6=CC=CC=C6)C=C4)[S](=O)(=O)C(F)(F)F)C1)C7=CC=C(Cl)C=C7
Molecular Weight 974.61

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

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

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