Agatolimod sodium - CAS 541547-35-7
Catalog number: 541547-35-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C238H291N75Na23O127P23S23
Molecular Weight:
8212.89
COA:
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Targets:
Toll-like Receptor (TLR)
Description:
Agatolimod sodium selectively targets Toll-like receptor 9 (TLR9). It has potential antineoplastic and immunostimulatory activity and is used as an anticancer adjuvant and immunostimulant.
Purity:
98%
Appearance:
Solid powder
Synonyms:
ProMune CpG 7909;CpG oligodeoxynucleotide 7909;CpG 2006;AV7909;PF3512676;PF-3512676;P-Thiothymidylyl-(3'-5')-2'-deoxy-P-thiocytidylyl-(3'-5')-2'-deoxy-P- thioguanylyl-(3'-5')-P-thiothymidylyl-(3'-5')-2'-deoxy-P-thiocytidylyl-(3'-5')- 2'-deoxy-P-thioguanyl
Solubility:
Soluble in DMSO, not in water
Storage:
-20°C Freezer
MSDS:
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Application:
Agatolimod sodium has potential antineoplastic and immunostimulatory activity and is used as an anticancer adjuvant and immunostimulant.
Quality Standard:
In-house standard
Quantity:
Milligrams-Grams
InChIKey:
YSQDQEOIFWWVHA-UHFFFAOYSA-A
InChI:
InChI=1S/C238H314N75O127P23S23.23Na/c1-93-49-294(225(334)266-191(93)244)167-31-115(424-450(357,473)376-69-139-116(32-168(400-139)295-50-94(2)192(245)267-226(295)335)425-451(358,474)379-72-142-120(36-172(403-142)299-54-98(6)196(249)271-230(299)339)429-456(
Canonical SMILES:
CC1=CN(C(=O)NC1=O)C2CC(C(O2)COP(=S)([O-])OC3CC(OC3COP(=S)([O-])OC4CC(OC4COP(=S)([O-])OC5CC(OC5COP(=S)([O-])OC6CC(OC6COP(=S)([O-])OC7CC(OC7COP(=S)([O-])OC8CC(OC8COP(=S)([O-])OC9CC(OC9COP(=S)([O-])OC1CC(OC1COP(=S)([O-])OC1CC(OC1COP(=S)([O-])OC1CC(OC1COP(=S)
1.Paclitaxel reduces regulatory T cell numbers and inhibitory function and enhances the anti-tumor effects of the TLR9 agonist PF-3512676 in the mouse.
Vicari AP;Luu R;Zhang N;Patel S;Makinen SR;Hanson DC;Weeratna RD;Krieg AM Cancer Immunol Immunother. 2009 Apr;58(4):615-28. doi: 10.1007/s00262-008-0586-2. Epub 2008 Sep 19.
The anti-tumor properties of Toll-like receptor (TLR) 9 agonist CpG oligodeoxynucleotides (ODN) are enhanced by combinations with several cytotoxic chemotherapy regimens. The mechanisms of this added benefit, however, remain unclear. We now report that, similar to the depletion of regulatory T cells (Treg) using anti-CD25, paclitaxel increased the anti-tumor effect of the TLR9 agonist PF-3512676 in a CD8(+) T cell-dependent fashion. Paclitaxel treatment decreased Treg numbers in a TLR4-independent fashion, and preferentially affected cycling Treg expressing high levels of FoxP3. The paclitaxel-induced reduction in Treg FoxP3 expression was associated with reduced inhibitory function. Adoptively transferred tumor-antigen specific CD8(+) T cells proliferated better in mice treated with paclitaxel and their recruitment in the tumor was increased. However, the systemic frequency of PF-3512676-induced tumor-antigen specific effector CD8(+) T cells decreased with paclitaxel, suggesting opposite effects of paclitaxel on the anti-tumor response. Finally, gene expression profiling and studies of tumor-associated immune cells revealed a complex modulation of the PF-3512676-induced immune response by paclitaxel, including a decrease of IL-10 expression and an increase in IL-17-secreting CD4(+) T cells.
2.Randomized phase 2/3 trial of CpG oligodeoxynucleotide PF-3512676 alone or with dacarbazine for patients with unresectable stage III and IV melanoma.
Weber JS;Zarour H;Redman B;Trefzer U;O'Day S;van den Eertwegh AJ;Marshall E;Wagner S Cancer. 2009 Sep 1;115(17):3944-54. doi: 10.1002/cncr.24473.
BACKGROUND: ;The primary objective of this phase 2 study was to assess the objective response rate (complete response [CR] + partial responses [PR]), by Response Evaluation Criteria in Solid Tumors, of PF-3512676, a CpG oligodeoxynucleotide, alone in 2 doses or in combination with dacarbazine (DTIC) in patients with unresectable stage IIIB/C or stage IV malignant melanoma, with the aim of selecting an arm to take forward to a phase 3 portion of the study.;METHODS: ;A total of 184 patients were randomized to 1 of 4 treatments: PF-3512676 10 mg (low dose), at 40 mg (high dose), 40 mg plus DTIC (850 mg/m(2)), or DTIC (850 mg/m(2)) alone. Patients received PF-3512676 subcutaneously weekly in a 3-week cycle and received DTIC intravenously on the first week of the cycle.;RESULTS: ;The objective response rate (PR or CR, confirmed or unconfirmed) in the 40 mg + DTIC arm was 16% (7 patients) compared with 8% (3 patients) with DTIC alone. One (2%) patient in the 10-mg and 0 patients in the 40-mg arms achieved an objective response. Best response of CR or PR or stable disease (SD), with no minimum duration defined for SD, was achieved by 15 (33%) patients in the 40 mg + DTIC arm, 15 (38%) patients in the DTIC-only arm, 8 (17%) patients in the 10-mg arm, and 9 (20%) patients in the 40-mg arm.
3.Intradermal CpG-B activates both plasmacytoid and myeloid dendritic cells in the sentinel lymph node of melanoma patients.
Molenkamp BG;van Leeuwen PA;Meijer S;Sluijter BJ;Wijnands PG;Baars A;van den Eertwegh AJ;Scheper RJ;de Gruijl TD Clin Cancer Res. 2007 May 15;13(10):2961-9.
PURPOSE: ;A decrease in the frequency and activation state of dendritic cells in the sentinel lymph node (SLN) has been observed in early stages of melanoma development. This may hinder the generation of effective antitumor T-cell responses and increase the likelihood of metastatic spread. Immunopotentiation of the melanoma SLN may therefore be a valuable adjuvant treatment option. One way to achieve this is through the use of bacterially derived unmethylated cytosine-phosphate-guanine (CpG) DNA sequences that bind Toll-like receptor 9 and activate plasmacytoid dendritic cells (PDC). CpG-activated PDC, in turn, release IFN alpha and may thus boost T-cell and natural killer cell responses as well as activate conventional myeloid dendritic cells (MDC).;EXPERIMENTAL DESIGN: ;We studied the effects of preoperative local administration of the CpG B-type oligodeoxynucleotide (ODN) PF-3512676 (formerly known as CPG 7909) on dendritic cell and T-cell subsets in the SLN of 23 stage I to III melanoma patients, randomized to receive intradermal injections of either PF-3512676 or saline (NaCl 0.9%).;RESULTS: ;PF-3512676 administration resulted in bulkier SLN, higher yields of isolated SLN leukocytes, and activation of BDCA-2(+)CD123(+) PDC as well as of CD1a(+) MDC.
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