Products

CP-690,550 is a potent and selective JAK inhibitor currently in clinical trials for rheumatoid arthritis (RA) and

other autoimmune disease indications. In enzyme assays it potently inhibited recombinant human kinase

protein JAK1 (IC50=3.2nM), JAK2 (IC50=4.1nM) and JAK3 (IC50=1.6nM), but in cellular assays it potently

inhibited signaling through JAK1 and JAK3 with 5-100 fold selectivity over JAK2.

Chemical Formula:

C₁₆H₂₀N₅O

CAS No.:

477600-75-2

Molecular Weight:

312.38

Purity:

> 98%

Appearance:

White solid

Chemical Name:

3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino) piperidin-

1-yl)-3-oxopropanenitrile

Solubility:

Up to 100 mM in DMSO

Storage:

For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution

at -20^oC.

Reference:

1. Meyer DM, et al. Anti-inflammatory activity and neutrophil reductions mediated by the JAK1/JAK3 inhibitor,

   CP-690,550, in rat adjuvant-induced arthritis. J Inflamm (Lond). 2010 11;7:41.

2. Flanagan ME, et al. Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the

   treatment of autoimmune diseases and organ transplant rejection. J Med Chem. 2010 53(24):8468-84

Cyclophosphamide, an immunosuppressant administered either orally or intravenously, is an antineoplastic

prodrug metabolized by P450 enzymes to phosphoramide mustard and acrolein which in turn alkylate DNA

and proteins, respectively. It is widely used in the treatment of chronic lymphocytic leukemia, lymphomas,

and soft tissue and osteogenic sarcomas.

Cyclophosphamide was shown to induce apoptosis in wt 9L gliosarcoma cells that did not express Bcl-2.

Bcl-2 diminishes cyclophosphamide's cytotoxic activity, but not cytostatic activity

Chemical Formula:

C₇H₁₅Cl₂N₂O₂P.H₂O

CAS No.:

6055-19-2

Molecular Weight:

261.09

Purity:

> 99%

Appearance:

White Crystalline

Chemical Name:

(RS)-N,N-bis(2-chloroethyl)-1,3,2-oxazaphosphinan-2-amine 2-oxide

Solubility:

Up to 100 mM in DMSO

Synonyms:

Cyclophosphamide, Endoxan, Cytoxan, Neosar, procytox, Revimmune, Cytophosphane

Storage:

For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution

at -20^oC.

Reference:

1. Schwartz et al., Cyclophosphamide induces caspase 9-dependent apoptosis in 9L tumor cells. Mol.

    Pharmcol. 2001, 60(6), 1268-1279.

2. Cyclophosphamide IARC monograph

FTY720, also named Fingolimod (trade name Gilenya), is an Immunomodulating drug approved by FDA in

2010 for treating multiple sclerosis. FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the

Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine. It is a novel immune modulator

that prolongs allograft transplant survival in numerous models by inhibiting lymphocyte emigration from

lymphoid organs. FTY720 is phosphorylated by sphingosine kinase, which then acts as a potent agonist at

four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). Down-regulation of

S1P1 receptors on T and B lymphocytes by FTY720 results in defective egress of these cells from spleen,

lymph nodes, and Peyer’s patch. FTY720 also enhances the activity of the sphingosine transporter Abcb1

and the leukotriene C4 transporter Abcc1 and inhibits cytosolic phospholipase A2 activity.

Chemical Formula:

C₁₉H₃₃NO₂

CAS No.:

162359-55-9

Molecular Weight:

307.47

Purity:

> 98%

Appearance:

White solid

Chemical Name:

2-amino-2-(4-octylphenethyl)propane-1,3-diol

Solubility:

Up to 100 mM in DMSO

Storage:

For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution

at -20^oC.

Reference:

1. Volker Brinkmann, et al. Fingolimod (FTY720): discovery and development of an oral drug to treat multiple

   sclerosis. Nature Reviews Drug Discovery 2010; 9, 883-897.

2. Brinkmann, V. et al. FTY720: Altered lymphocyte traffic results in allograft protection. Transplantation, 2001;

   72 764-769.

3. Brinkmann, V. et al. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. J Biol

   Chem, 2002; 277(24) 21453-21457.

4. Matloubian, M. et al. Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on

   S1P receptor 1. Nature, 2004; 427 355-360.

5. Honig, S.M. et al. FTY720 stimulates multidrug transporter- and cysteinyl leukotriene-dependent T cell

  chemotaxis to lymph nodes. J Clin Invest, 2003; 111(5) 627-637.

6. Payne, S.G. et al. The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2

   independently of sphingosine-1-phosphate receptors. Blood, 2007; 109(3) 1077-1085.

Leukadherin-1 (LA1), a novel small molecule agonist of integrin CD11b/CD18, can increase the extent of

CD11b/CD18-dependent cell adhesion of transfected cells and of primary human and mouse neutrophils

(EC50 =4µM in vitro), which resulted in decreased chemotaxis and transendothelial migration. LA1 can also

decrease leukocyte recruitment and reduced arterial narrowing after injury in rats. Moreover, compared to a

known integrin antagonist, LA1 preserved kidney function better in a mouse model of experimental nephritis.

It inhibited leukocyte recruitment by increasing leukocyte adhesion to the inflamed endothelium, which was

reversed with a blocking antibody.

Chemical Formula:

C₂₂H₁₅NO₄S₂

CAS No.:

344897-95-6

Molecular Weight:

421.49

Purity:

> 98%

Appearance:

White solid

Chemical Name:

(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid

Solubility:

Up to 50 mM in DMSO

Storage:

For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution

at -20^oC.

Reference:

1. Dony Maiguel, et al. Small Molecule–Mediated Activation of the Integrin CD11b/CD18 Reduces

    Inflammatory Disease. Sci. Signal., Vol. 4, Issue 189, p. ra57

2. Faridi MH et al. Identification of novel agonists of the integrin CD11b/CD18. Bioorg Med Chem Lett. 2009; 19

   (24):6902-6.