500507 Sigma-AldrichCXCR4 Antagonist IV, TF14016 - Calbiochem

CXCR4 Antagonist IV, TF14016 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

SDS
References
Data Sheet

Synonyms: Fusin Antagonist IV

Primary Target: CXCR4

Recommended Products

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O

Pricing & Availability

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Description
Overview	A 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-1_IIIB 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 Number	500507
Brand Family	Calbiochem®
Synonyms	Fusin Antagonist IV

References
References	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.

Product Information
Form	White solid
Formulation	Supplied as a trifluoroacetate salt.
Hill Formula	C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
Chemical formula	C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
Quality Level	MQ100

Applications

Biological Information
Primary Target	CXCR4
Primary Target IC<sub>50</sub>	0.9 nM
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y
Peptide Sequence	N^α-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 Instructions	Following 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.

Revision	31-May-2013 JSW
Synonyms	Fusin Antagonist IV
Description	A 14-aa internally disulfide-bonded peptide that potently protects MT-4 cells against X4-HIV strain HIV-1_IIIB 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).
Form	White solid
Formulation	Supplied as a trifluoroacetate salt.
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₁₀₁H₁₄₅FN₃₄O₁₈S₂.xH₂O
Peptide Sequence	N^α-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
Solubility	H₂O (100 mg/ml)
Storage	-20°C Protect from light
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	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.