1. Immunology/Inflammation
  2. Transmembrane Glycoprotein Interleukin Related
  3. KHK2840

KHK2840 是一种强效的 CD40 激动剂,对 hCD40 的 Kd 值为 0.485 nM。KHK2840 可在荷瘤 hCD40 转基因小鼠和人外周血 B 细胞中传递激动信号。KHK2840 可上调 CD80CD86CD95IL-12p70 的表达。KHK2840 可增强抗 PD-1 抗体和 Paclitaxel (HY-B0015) 的抗肿瘤功效。KHK2840 可用于癌症相关研究,例如结肠癌和黑色素瘤。

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KHK2840

KHK2840 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KHK2840 is a potent CD40 agonist with a Kd value of 0.485 nM for hCD40. KHK2840 delivers agonistic signals in tumor-bearing hCD40 transgenic mice and human peripheral blood B cells. KHK2840 upregulates CD80, CD86, CD95 and IL-12p70 expression. KHK2840 enhances antitumor efficacy of anti-PD-1 antibody and Paclitaxel (HY-B0015). KHK2840 can be used for the research of cancer, such as colon cancer and melanoma[1].

同型

Human IgG2 kappa

推荐同型对照抗体
反应种属

Human

IC50 & Target[1]

IL-12

 

体外研究
(In Vitro)

KHK2840 (0.0625-1.00 μg/mL) 可特异性结合人食蟹猴 CD40 蛋白 (人源蛋白的 Kd = 0.485 nM;食蟹猴源蛋白的 Kd = 1.46 nM),但不结合大鼠或小鼠的 CD40 蛋白[1]
KHK2840 (2 天) 可激活人单核细胞来源的树突状细胞,上调 CD80、CD86 和 IL-12p70 的表达 (CD80 的 EC50 = 0.188 μg/mL,CD86 的 EC50 = 0.072 μg/mL,IL-12p70 的 EC50 = 0.436 μg/mL)[1]
KHK2840 (0.01-10 μg/mL;0.5-48 h) 以浓度和时间依赖的方式上调 CD86 和 CD95 的表达[1]
KHK2840 (过夜处理) 在人外周血 B 细胞中诱导 CD69、CD86 和 CD95 表达 (CD69 对应的 EC50 = 0.018 μg/mL,CD86 对应的 EC50 = 0.015 μg/mL,CD95 对应的 EC50 = 0.016 μg/mL)[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Cynomolgus Monkey[1] 0.1 mg/kg i.v. Cmax 2.13 (Male) μg/mL
Cynomolgus Monkey[1] 0.1 mg/kg i.v. Vss 68.8 (Male) mL/kg
Cynomolgus Monkey[1] 0.1 mg/kg i.v. Cmax 2.75 (Female) μg/mL
Cynomolgus Monkey[1] 0.1 mg/kg i.v. Vss 52.7 (Female) mL/kg
Cynomolgus Monkey[1] 0.3 mg/kg i.v. Cmax 6.64 (Male) μg/mL
Cynomolgus Monkey[1] 0.3 mg/kg i.v. Vss 60.9 (Male) mL/kg
Cynomolgus Monkey[1] 0.3 mg/kg i.v. Cmax 9.10 (Female) μg/mL
Cynomolgus Monkey[1] 0.3 mg/kg i.v. Vss 35.3 (Female) mL/kg
Cynomolgus Monkey[1] 1 mg/kg i.v. Cmax 25.6 (Male) μg/mL
Cynomolgus Monkey[1] 1 mg/kg i.v. Vss 45.3 (Male) mL/kg
Cynomolgus Monkey[1] 1 mg/kg i.v. Vss 55.7 (Female) mL/kg
Cynomolgus Monkey[1] 3 mg/kg i.v. Cmax 73.1 (Male) μg/mL
Cynomolgus Monkey[1] 3 mg/kg i.v. Vss 40.8 (Male) mL/kg
Cynomolgus Monkey[1] 3 mg/kg i.v. Cmax 78.9 (Female) μg/mL
Cynomolgus Monkey[1] 3 mg/kg i.v. Vss 38.7 (Female) mL/kg
体内研究
(In Vivo)

KHK2840 (0.038-1.2 mg/kg;静脉注射;单剂量) 在患有结肠癌、黑色素瘤或胰腺导管腺癌模型的雌性 hCD40 BAC 转基因小鼠中,表现出剂量依赖性的 CD40 激动活性和抗肿瘤功效[1]
KHK2840 (0.1-3 mg/kg;静脉注射;每 2 周 1 次;共 3 剂) 可在食蟹猴雌雄个体中诱导呈剂量依赖性的 CD40 激动信号 (其无可见有害作用水平 (NOAEL) 为 0.3 mg/kg)[1]

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

Animal Model: hCD40 BAC transgenic mice with colon cancer, melanoma, or pancreatic ductal adenocarcinoma models (female, C57Bl/6J background)[1]
Dosage: 0.038, 0.075, 0.15, 0.3, 0.6, 1.2 mg/kg
Administration: I.v.; single dose
Result: Significantly suppressed MC-38 tumor growth (P=0.0128) with 1.2 mg/kg monotherapy.
Achieved significant tumor growth suppression.
Induced tumor remission in 8/10 mice in pancreatic cancer model when combined with anti-PD-1.
Observed dose-dependent increases in CD80-, CD86-, CD95- positive B cells and cytokines (IL-12p70, IFN-γ, IL-6, IL-10, TNF-α, IL-1β, CXCL1) in peripheral blood.
Increased cell type scores of Th1 cells (lymph nodes), DCs (tumors/lymph nodes), and CD8 T cells (tumors).
基因 ID

958  [NCBI]

Accession
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.

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
KHK2840
目录号:
HY-P991918
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