[CAS NO. 1260251-31-7]  Birinapant (TL32711)

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PRODUCTS SPECIFICATIONS [1260251-31-7]

Catelog
SLK-S7015
Brand
Selleck
CAS
1260251-31-7

DESCRIPTION [1260251-31-7]

Overview

MDL-
Molecular Weight806.94
Molecular FormulaC42H56F2N8O6
SMILES-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.2392 mL6.1962 mL12.3925 mL
5 mM0.2478 mL1.2392 mL2.4785 mL
10 mM0.1239 mL0.6196 mL1.2392 mL
50 mM0.0248 mL0.1239 mL0.2478 mL

Description

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to with of <1 nM in a cell-free assay, less potent to XIAP. Birinapant helps to induce in latent HIV-1-infected cells. Phase 2.

Targets

cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
<1 nM(Kd)45 nM(Kd)

In vitro

Birinapant binds with XIAP and cIAP1 with K of 45 and <1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.

In vivo

Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with.