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Plerixafor (hydrochloride hydrate)

Cayman Chemical Item Number 10011332

Mobozil™; SID 791; JM 3100; AMD 3100 (CAS 155148-31-5)

Plerixafor (hydrochloride hydrate) (CAS 155148-31-5)

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Description

The α-chemokine receptor, CXCR4, on CD4+ T-cells is used by CXCR4-selective HIV forms as a gateway for T-cell infection. In mammalian cell signaling, CXCR4 activation promotes the homing of hematopoietic stem cells, chemotaxis and quiescence of lymphocytes, and growth and metastasis of certain cancer cell types. Plerixafor (hydrochloride) is a macrocyclic compound that acts as an irreversible antagonist against the binding of CXCR4 with its ligand, SDF-1 (CXCL12). It suppresses infection by HIV with an IC50 value of 1-10 ng/ml1 with selectivity toward CXCR4-tropic virus.2 Plerixafor mobilizes hematopoietic stem and progenitor cells for transplant3 better than the 'gold standard', G-CSF alone 4 and synergizes with G-CSF.3 It also increases T-cell trafficking in the blood and spleen5 as well as the central nervous system.6 Plerixafor regulates the growth of primary and metastic breast cancer cells7 and inhibits dissemination of ovarian carcinoma cells.8

1 De Clercq, E., Yamamoto, N., Pauwels, R., et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother 38(4) 668-674 (1994).

2 Fransen, S., Bridger, G., Whitcomb, J.M., et al. Supression of dualtropic human immunodeficiency virus type 1 by the CXCR4 antagonist AMD3100 is associated with efficiency of CXCR4 use and baseline virus composition. Antimicrob Agents Chemother 52(7) 2608-2615 (2008).

3 Broxmeyer, H.E., Orschell, C.M., Clapp, D.W., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med 201(8) 1307-1318 (2005).

4 Hess, D.A., Bonde, J., Craft, T.C., et al. Human progenitor cells rapidly mobilized by AMD3100 repopulate NOD/SCID mice with increased frequency in comparison to cells from the same donor mobilized by granulocyte colony stimulating factor. Biol Blood Marrow Transplant 13 398-411 (2007).

5 Bernardini, G., Sciumè, G., Bosisio, D., et al. CCL3 and CXCL12 regulate trafficking of mouse bone marrow NK cell subsets. Blood 111(7) 3626-3634 (2008).

6 McCandless, E.E., Zhang, B., Diamond, M.S., et al. CXCR4 antagonism increases T cell trafficking in the central nervous system and improves survival from west nile virus encephalitis. Proc Natl Acad Sci USA 105(32) 11270-11275 (2008).

7 Smith, M.C.P., Luker, K.E., Garbow, J.R., et al. CXCR4 regulates growth of both primary and metastatic breast cancer. Cancer Res 64 8604-8612 (2004).

8 Kajiyama, H., Shibata, K., Terauchi, M., et al. Involvement of SDF-1a/CXCR4 axis in the enhanced peritoneal metastasis of epithelial ovarian carcinoma. Int J Cancer 122 91-99 (2008).

Synonyms
  • Mobozil™
  • SID 791
  • JM 3100
  • AMD 3100
Formal Name 1,​4-​bis((1,​4,​8,​11-​tetraazacyclotetradecan-​1-​yl)methyl)benzene,​ octahydrochloride
CAS Number 155148-31-5
Molecular Formula C28H54N8 · 8HCl · [XH2O]
Formula Weight 794.5
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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N1CCCNCCN(CCCNCC1)​Cc1ccc(cc1)​CN1CCCNCCNCCCNCC1

Background Reading

De Clercq, E., Yamamoto, N., Pauwels, R., et al. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100. Antimicrob Agents Chemother 38(4) 668-674 (1994).

Fransen, S., Bridger, G., Whitcomb, J.M., et al. Supression of dualtropic human immunodeficiency virus type 1 by the CXCR4 antagonist AMD3100 is associated with efficiency of CXCR4 use and baseline virus composition. Antimicrob Agents Chemother 52(7) 2608-2615 (2008).

Broxmeyer, H.E., Orschell, C.M., Clapp, D.W., et al. Rapid mobilization of murine and human hematopoietic stem and progenitor cells with AMD3100, a CXCR4 antagonist. J Exp Med 201(8) 1307-1318 (2005).

Hess, D.A., Bonde, J., Craft, T.C., et al. Human progenitor cells rapidly mobilized by AMD3100 repopulate NOD/SCID mice with increased frequency in comparison to cells from the same donor mobilized by granulocyte colony stimulating factor. Biol Blood Marrow Transplant 13 398-411 (2007).

Bernardini, G., Sciumè, G., Bosisio, D., et al. CCL3 and CXCL12 regulate trafficking of mouse bone marrow NK cell subsets. Blood 111(7) 3626-3634 (2008).

McCandless, E.E., Zhang, B., Diamond, M.S., et al. CXCR4 antagonism increases T cell trafficking in the central nervous system and improves survival from west nile virus encephalitis. Proc Natl Acad Sci USA 105(32) 11270-11275 (2008).

Smith, M.C.P., Luker, K.E., Garbow, J.R., et al. CXCR4 regulates growth of both primary and metastatic breast cancer. Cancer Res 64 8604-8612 (2004).

Kajiyama, H., Shibata, K., Terauchi, M., et al. Involvement of SDF-1a/CXCR4 axis in the enhanced peritoneal metastasis of epithelial ovarian carcinoma. Int J Cancer 122 91-99 (2008).

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Size Price Quantity Subtotal
1 mg $13.00 $0.00
5 mg $59.00 $0.00
10 mg $104.00 $0.00
50 mg $455.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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