2. Immunology/Inflammation
  3. Scavenger Receptor Class B type I (SR-BI）
  4. PLT012

PLT012 是一种靶向 CD36 的人源化 IgG4 抗体。PLT012 抑制 CD36 的脂质结合结构域。PLT012 通过阻断调节性 T 细胞和CD8+ 肿瘤浸润淋巴细胞中 CD36 介导的代谢适应，从而抑制肿瘤生长，并将肿瘤微环境从免疫抑制状态转变为免疫支持状态。PLT012 能减少瘤内 Tregs，增强 CD8+ T 细胞的浸润和细胞毒功能，并增加祖细胞耗竭 T 细胞的丰度。PLT012 能发挥强大的抗肿瘤活性，并与抗 PD-L1 或与抗 VEGF + 抗 PD-L1 产生协同作用。PLT012 可用于肝细胞癌、结直肠癌及实体瘤的相关研究。

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PLT012

PLT012 Chemical Structure

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PLT012 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLT012 is a humanized IgG4 antibody targeting CD36. PLT012 inhibits the lipid-binding domain of CD36. PLT012 blocks CD36-mediated metabolic adaptation in regulatory T cells (Tregs) and CD8+ tumor-infiltrating lymphocytes (TILs), thereby inhibiting tumor growth and shifting the tumor microenvironment from immunosuppressive to immunosupportive. PLT012 reduces intratumoral Tregs, enhances CD8+ T cell infiltration and cytotoxic function, and increases the abundance of progenitor-exhausted T cells. PLT012 exerts robust antitumor activity and synergizes with anti-PD-L1 or standard-of-care regimens (anti-VEGF + anti-PD-L1). PLT012 can be used for hepatocellular carcinoma, colorectal cancer and solid tumor research[1].

反应种属

Human
IC50 & Target[1]

CD36

 

体外研究
(In Vitro)

PLT012 (0.001-100 μg/mL，30 分钟) 能强烈抑制荧光标记的氧化低密度脂蛋白 (oxLDL) 在过表达人CD36 的 F293 细胞中的结合 (IC50 = 1.798 nM) 和摄取 (IC50 = 1.357 nM)[1]。
PLT012 (5 mg/mL，30 分钟) 显著抑制从 MC38 荷瘤小鼠分离的原代肿瘤浸润免疫细胞 (包括髓系细胞、CD3+T 淋巴细胞及瘤内调节性 T 细胞) 对 oxLDL 的摄取[1]。
PLT012 通过单细胞 RNA 测序技术分析分离的 CD45+ 肿瘤浸润细胞，恢复耗竭 T 细胞的效应功能，并诱导 CD8+ T 细胞介导的抗肝癌反应[1]。
PLT012 (2 天) 通过靶向 CD36，在人类肝癌组织中有效调节肿瘤微环境[1]。

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

PLT012 相关抗体:
体内研究
(In Vivo)

PLT012 在 Yumm1.7 黑色素瘤和 MC38 结直肠癌模型中均展现出良好的抗肿瘤反应[1]。
PLT012 (10 mg/kg，单次腹腔注射) 在CTNNB1N90/MYCOE HCC荷瘤小鼠中，可能通过靶向 CD36 介导的免疫调节，恢复抗肝癌免疫[1]。
PLT012 (10 mg/kg，腹腔注射，每三天一次，持续 18 天) 在MYCOE/p53KO HCC小鼠模型中，能够恢复抗肿瘤反应，并可能提高对 PD-1 阻断疗法的应答[1]。
PLT012 (10 mg/kg，腹腔注射，每三天一次，共 5 次) 在CTNNB1N90/MYCOE HCC荷瘤小鼠中，可重塑 β-catenin 突变型肝癌的免疫抑制性肿瘤微环境，有效激活抗肿瘤 T 细胞免疫[1]。
PLT012 在 CTNNB1N90/MYCOE HCC 荷瘤小鼠中，与抗 PD-L1 单抗或抗 VEGF 联合抗 PD-L1 联用时，能显著增强抗肿瘤疗效；当与抗 PD-L1 及抗 VEGF 三联联用时，可获得 >70% 的总阳性反应率和 45% 的完全缓解率[1]。
PLT012 在 CTNNB1N90/MYCOE HCC 荷瘤小鼠中，无论饲喂标准普通饲料还是高脂西式饮食，均能抑制高膳食脂质摄入条件下的肝癌进展[1]。
PLT012 可重编程肿瘤免疫微环境，从而限制结肠癌肝转移，并增强小鼠 MC38 移植瘤模型对 PD-1 阻断的敏感性[1]。
PLT012 (0-200 mg/kg，每周一次，持续五周) 在非人灵长类动物 (食蟹猴) 中耐受性良好[1]。

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

Animal Model: C57BL/6 mice (6 weeks) (received 12 μg of pT3-b-catenin, 12 μg of pT3-Myc_LucOVA plasmid, and 8 μg of SB100x)[1]
Dosage: 10 mg/kg
Administration: i.p. once
Result: Mainly accumulated in the liver, lung, intestine, epididymal white adipose tissue, and pancreas.
Showed average fluorescence intensity levels because of the presence of adipocytes and endothelial cells.
Significantly stronger in livers after 24 h.
Resulted a higher percentage of labeled cells in both Tregs and CD8+ T cells after persisted for 48 h.
Resulted a higher signal in NK cells at the 24 h but not at the 48 h.
Animal Model: C57BL/6 mice (6 weeks) (received a total of 12 μg of pT3-Myc_LucOVA plasmid, 13.2 μg of p53 gRNA plasmid, and 4 μg of SB100x) [1]
Dosage: 10 mg/kg
Administration: i.p. once every three days, 18 days
Result: Inhibited the growth of MYCOE/p53KO HCC and led to complete tumor regression in 32% of tumor-bearing mice (this finding was further corroborated by measurements of tumor weight and ex vivo liver bioluminescence imaging).
Reduced serum alanine transaminase (ALT) activity.
Led to a reduction of Tregs and an increase of CD8+ T cells within the TME.
Resulted a higher CD8+ T/Tregs ratios.
Enhanced the abundance of CD8+ GrB+ T cells.
Resulted in an increase in both progenitor-exhausted T cells (Prog Tex, characterized by CD44+ PD-1+ TCF1+ Tim3-) and terminally exhausted T cells (Term Tex, characterized by CD44+ PD-1+ TCF1- Tim3+).
Animal Model: C57BL/6 mice (6 weeks) (received 12 μg of pT3-b-catenin, 12 μg of pT3-Myc_LucOVA plasmid, and 8 μg of SB100x)[1]
Dosage: 10 mg/kg
Administration: i.p. once every three days for 5 doses
Result: Significantly inhibited tumor growth and markedly decreased circulating ALT levels.
Also increased the abundance of CD8+ T cells and decreased the proportion of Tregs, thereby resulting in increased ratios of CD8+ T cells to Tregs within individual tumors.
Increased the abundance of GrB-expressing CD8+ T cells as well as the population of Prog Tex and Term Tex CD8+ T cells.
Observed a stronger signal for GrB and cleaved caspase-3 in tumors.
Significantly enhanced the antigen-specific T cell response.
Increased frequencies of antigen-specific Prog Tex and Term Tex in CD8+ T cells.
基因 ID

948  [NCBI]

Accession

P16671-1
应用

ELISA, FACS, Functional assay
偶联物

Unconjugated
复溶方法

The product can be reconstituted/diluted with sterile PBS or saline.
组分

Please refer to the lot-specific COA for specific buffer information.
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

PLT012 相关分类

  • 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.

Keywords:

PLT012PLT 012PLT-012Scavenger Receptor Class B type I (SR-BI）Scavenger receptor class B member 1SRB1CD36 and LIMPII analogous 1 (CLA-1)CD36 antigen-like 1humanized IgG4 antibodymicroenvironmenthepatocellular carcinomacolorectal cancersolid tumorInhibitorinhibitorinhibit

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