500507 CXCR4 Antagonist IV, TF14016 - Calbiochem

500507
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O

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      Glass bottle 2 mg
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      Description
      OverviewA 14-aa internally disulfide-bonded peptide that potently competes against SDF-1α/CXCL12 for CXCR4 binding (IC50 = 0.91 nM; [SDF-1] = 100 nM) and protects MT-4 cells against X4-HIV strain HIV-1IIIB infection (EC50 = 4 nM in 5 d; MOI = 0.01) with no significant cytotoxicity (CC50 = 56 µM; 5 d). Inhibits SDF-1-induced Ca2+ mobilization (IC50 = 4.5 nM; [SDF-1] = 30 nM; CXCR4-expressing CHO cells) in vitro and effectively prevents CXCR4-dependent 5BC-5 metastasis in NK-depleted SCID mice in vivo (10 mg/kg i.p.) in vivo.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number500507
      Brand Family Calbiochem®
      SynonymsFusin Antagonist IV
      References
      ReferencesOtani, Y., et al. 2012. FEBS Lett. 586, 3639.
      Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem. 10, 5720.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1 3663.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1, 3656.
      Product Information
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Hill FormulaC₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
      Chemical formulaC₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetCXCR4
      Primary Target IC<sub>50</sub>0.9 nM
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Peptide SequenceNα-4-fluorobenzoyl-Arg-Arg-Nal-Cys⁴-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys¹³-Arg-NH₂ (Disulfide bond: 4 → 13; Nal = L-3-(2-naphthyl)alanine; Cit = L-citrulline)
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      CXCR4 Antagonist IV, TF14016 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Otani, Y., et al. 2012. FEBS Lett. 586, 3639.
      Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem. 10, 5720.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1 3663.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1, 3656.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision31-May-2013 JSW
      SynonymsFusin Antagonist IV
      DescriptionA 14-aa internally disulfide-bonded peptide that potently protects MT-4 cells against X4-HIV strain HIV-1IIIB infection (EC50 = 4 nM in 5 d; MOI = 0.01) by competing against SDF-1α/CXCL12 for CXCR4 binding (IC50 = 0.91 nM; [SDF-1] = 100 nM; CXCR4-expressing CHO cells), while exhibiting cytotoxicity only at much higher concentrations (CC50 = 56 µM; 5 d in MT-4 cultures by MTT assays). Shown to inhibit SDF-1-induced Ca2+ mobilization (IC50 = 4.5 nM; [SDF-1] = 30 nM; CXCR4-expressing CHO cells) and cell migration (1.01- and 1.41-fold of non-SDF-1-stimulated control, respectively, with or without 100 nM TF14016; [SDF-1] = 100 ng/mL; 5BC-5 cells) in cultures in vitro and effectively prevent CXCR4-dependent SCLC (small lung cancer cell) 5BC-5 metastasis in NK-depleted SCID mice in vivo (average # of lung foci/nodules 12 wks after 5BC-5 i.v. inoculation = 1.25 vs. 9.75, respectively, with or without daily 10 mg/kg i.p. dosage).
      FormWhite solid
      FormulationSupplied as a trifluoroacetate salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
      Peptide SequenceNα-4-fluorobenzoyl-Arg-Arg-Nal-Cys⁴-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys¹³-Arg-NH₂ (Disulfide bond: 4 → 13; Nal = L-3-(2-naphthyl)alanine; Cit = L-citrulline)
      Purity≥95% by HPLC
      SolubilityH₂O (100 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesOtani, Y., et al. 2012. FEBS Lett. 586, 3639.
      Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem. 10, 5720.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1 3663.
      Tamamura, H., et al. 2003. Org. Biomol. Chem. 1, 3656.