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Birinapant

Cat. No. M2166
Birinapant Structure
Synonym:

TL32711

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 185 In stock
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Quality Control
Biological Activity

Birinapant (also known as TL32711) is a SMAC mimetic antagonist and an inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with antitumor activity in vivo. Birinapant has high binding affinity (nM range) for cIAP1/2 and XIAP. Birinapant (TL32711) caused rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. TL32711 (Birinapant) combined with TNF-α inhibited the growth of a melanoma cell line with acquired resistance to BRAF inhibition to the same extent as in the parental cell line. In addition, Birinapant in combination or as a single agent decreased colony formation and anchorage-independent growth potential of IBC cells. TL32711 is currently in a phase 2 single agent and combination clinical studies in solid tumors.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 806.94
Formula C42H56F2N8O6
CAS Number 1260251-31-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells.
Krepler C, et al. Clin Cancer Res. 2013 Apr 1;19(7):1784-94. PMID: 23403634.

Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism.
Allensworth JL, et al. Breast Cancer Res Treat. 2013 Jan;137(2):359-71. PMID: 23225169.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Birinapant, TL32711 supplier, IAP, inhibitors

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