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5.00507

Sigma-Aldrich

CXCR4 Antagonist IV, TF14016

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Synonym(s):
CXCR4 Antagonist IV, TF14016, Fusin Antagonist IV
Empirical Formula (Hill Notation):
C101H145FN34O18S2 · xH2O
Molecular Weight:
2206.58 (anhydrous basis)

assay

≥95% (HPLC)

Quality Level

form

solid

potency

0.9 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

H2O: 100 mg/mL

storage temp.

−20°C

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This Item
5.09374ABN1449C8352
vibrant-m

5.00507

CXCR4 Antagonist IV, TF14016

vibrant-m

5.09374

Fn14 Antagonist, L524-0366

vibrant-m

ABN1449

Anti-CXCR-4

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

200

form

solid

form

powder

form

-

form

buffered aqueous solution

assay

≥95% (HPLC)

assay

≥98% (HPLC)

assay

-

assay

-

solubility

H2O: 100 mg/mL

solubility

DMSO: 25 mg/mL

solubility

-

solubility

-

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-

storage condition

-

General description

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-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.
A 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).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
CXCR4

Warning

Toxicity: Standard Handling (A)

Sequence

Nα-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)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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