500507 CXCR4 Antagonist IV, TF14016 - Calbiochem

500507
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00507.0001
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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
          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

          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.