DSR-6434

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DSR-6434具有很强的抗肿瘤作用。 DSR-6434 是一种有效的选择性 Toll 样受体 7 (TLR7) 激动剂，对人和小鼠 TLR7 的 EC50 值分别为 7.2 nM 和 4.6 nM。

DSR-6434 has a strong antitumor effect. DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively.(In Vitro):To assess the specificity of DSR-6434 toward TLR7, an NF-κB-driven reporter assay is performed in HEK293 cells engineered to express either hTLR7, TLR8 or TLR9. In this assay, successful binding of DSR-6434 to the specific receptor leads to NF-κB activation. DSR-6434 is capable of stimulating reporter gene activity only in HEK293 cells expressing hTLR7 and not in HEK293 cells expressing the structurally similar hTLR8 or hTLR9.(In Vivo):In B6C3F1 mice, DSR-6434 (0.1-1 mg/kg; i.v.) significantly suppresses lung metastasis.

To assess the specificity of DSR-6434 toward TLR7, an NF-κB-driven reporter assay is performed in HEK293 cells engineered to express either hTLR7, TLR8 or TLR9. In this assay, successful binding of DSR-6434 to the specific receptor leads to NF-κB activation. DSR-6434 is capable of stimulating reporter gene activity only in HEK293 cells expressing hTLR7 and not in HEK293 cells expressing the structurally similar hTLR8 or hTLR9.

DSR-6434 treatment (Compound 20; 0.1-1 mg/kg; intravenous injection; biweekly; for 4 weeks; B6C3F1 mice) suppresses the lung metastasis significantly, 78% inhibition at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group). Animal Model:B6C3F1 mice injected with HM-1 ovarian cancer cells Dosage:0.1 mg/kg, 1 mg/kg Administration:Intravenous injection; biweekly; for 4 weeks Result:Suppressed the lung metastasis significantly, 78% inhibition was seen at 0.1 mg/kg dosing (with no tumor metastasis at the 1 mg/kg group).

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Others

Other Targets

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1059070-10-8

400.487

C19H28N8O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (312.13 mM)

CCCCNc1nc(N)c2[nH]c(=O)n(Cc3ccc(OCCN(C)C)nc3)c2n1

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(-20℃)

With Ice Pack

≥ 2 years