1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. SCL-1

SCL-1 是一种口服有效的抗 PD-1/PD-L1 抑制剂。SCL-1 能够抑制 PD-1/PD-L1 的结合。SCL-1 可增加 T 细胞、B 细胞和自然杀伤细胞的数量。SCL-1 具有强大的肿瘤生长抑制作用,其作用机制是通过在肿瘤内诱导效应 T 细胞,以及上调长链非编码 RNA 作为新抗原的表达,从而激活细胞毒性 T 淋巴细胞。SCL-1 可用于癌症研究,如三阴性乳腺癌。

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SCL-1

SCL-1 Chemical Structure

CAS No. : 1061105-16-5

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SCL-1 is an orally active anti-PD-1/PD-L1 inhibitor. SCL-1 can inhibit PD-1/PD-L1 binding. SCL-1 increases T cells, B cells and natural killer cells. SCL-1 exerts strong tumor growth inhibitory effects that were mediated by effector T-cell induction inside tumors and the up-regulated expression of long non-coding RNAs as neoantigens leading to cytotoxic T lymphocyte activation. SCL-1 can be used for the research of cancer, such as triple-negative breast cancer[1][2].

体外研究
(In Vitro)

SCL-1 (0.25-100 μM, 4 days) 对 MDA-MB231 细胞无显著细胞毒性[1]
SCL-1 (25 μM) 对 PD-1/PD-L1 结合具有中等抑制活性,抑制率为 63%[2]
SCL-1 可抑制 SCC3 和 Jurkat 细胞增殖,其 IC50 值均 >50 μM[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

SCL-1 (25-100 mg/kg,口服,14 天内给药 10 次) 可抑制人源化的 MDA-MB231 肿瘤负荷的 MHC-dKO NOG 小鼠中的肿瘤生长[1]
SCL-1 (50 mg/kg,口服,14 天内给药 10 次) 可抑制人源化 SCC-3 肿瘤负荷的 MHC-dKO NOG 小鼠中的肿瘤生长[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA-MB231 tumor in a humanized MHC-double knockout NOG mice models[1]
Dosage: 25, 50 and 100 mg/kg
Administration: Orally administered, 10 times over 14 days (days 1-5 and 8-12)
Result: Inhibited tumor volume.
Did not induce weight loss.
Increased infiltrated CD4+ and CD8+ T-cell numbers inside tumors.
Increased the frequency of CD19+ B cells that infiltrated tumors.
Showed high level of lymphoid cell infiltration.
Upregulated T cell-associated cytotoxic genes (GZMB, PRF1, and IFNB1), exhausted marker genes (PD-1, TIM3, and CD39), NK activation-associated genes (CD16 and NCR1), and T-cell attracting chemokine genes (CCL3 and CCL4).
Downregulated CXCL12 gene expression.
Upregulated tumor-specific long non-coding (lnc) RNAs.
Animal Model: Humanized SCC-3 tumor-bearing MHC-dKO NOG mice[2]
Dosage: 50 mg/kg
Administration: Orally administered, 10 times over 14 days (days 1-5 and 8-12)
Result: Promoted the engraftment of transplanted human PBMCs in the spleens.
Increased the number of infiltrated CD45+ human PBMCs and CD4+ and CD8+ T cells inside the tumors.
Had more foci of lymphoid cell infiltration with necrotic changes.
Increased CD8+ T cells.
Upregulated the expression of CXCL9 and CXCR3.
Downregulated the expression levels of CCL22 and TIM3.
分子量

396.41

Formula

C18H23F3N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SCL-1
目录号:
HY-175604
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