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      Birinapant (TL32711)
      Birinapant (TL32711)

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      This product is for research use only, not for human use. We do not sell to patients.
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      InvivoChem Cat #: V0051
      CAS #: 1260251-31-7Purity ≥98%

      Description: Birinapant (TL32711; TL-32711; TL 32711) is a novel and potent bivalent SMAC peptido-mimetic antagonist, mostly to cIAP1 with Kd of<1 nM in a cell-free assay, less potent to XIAP. Birinapant not only binds to the isolated BIR3 domains of cIAP1, cIAP2, XIAP but the single BIR domain of ML-IAP with high affinity and degrades TRAF2-bound cIAP1 and cIAP2 rapidly accordingly inhibiting the activation of TNF-mediated NF- kB. Additionally, birinapantcan promote the formation of caspase-8: RIPK1 complex in response to TNF stimulation, which result in downstream caspasesactivation.

      References: Breast Cancer Res Treat. 2013 Jan;137(2):359-71.

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      Molecular Weight (MW)806.94
      FormulaC42H56F2N8O6
      CAS No.1260251-31-7
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 100 mg/mL (123.9 mM)
      Water:<1 mg/mL (slightly soluble or insoluble)
      Ethanol: 55 mg/mL (68.1 mM)
      Solubility (In vivo)15% Captisol: 15mg/mL
      Chemical Name(2S,2'S)-N,N'-((2S,2'S)-((3S,3'S,5R,5'R)-5,5'-((6,6'-difluoro-1H,1'H-[2,2'-biindole]-3,3'-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide)


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      In VitroBirinapant binds with XIAP and cIAP1 with Kd 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(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.
      In VivoBirinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with.
      Animal modelHuman melanoma xenografts 451Lu
      Formulation & Dosage12.5% Captisol in distilled water; 30 mg/kg; i.p. 3 times per week 
      References[1] Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       

      Birinapant

      		 

      Birinapant

      Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.
      		 

      Birinapant

      Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.

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