1. Antibody-drug Conjugate/ADC Related Immunology/Inflammation Cell Cycle/DNA Damage Cytoskeleton
  2. Antibody-Drug Conjugates (ADCs) Transmembrane Glycoprotein Microtubule/Tubulin
  3. GLK-33

GLK-33 是一种靶向 CD33+ 的抗体药物偶联物 (ADC)。GLK-33 能与人源 CD33 及 CD33-Fc 融合蛋白结合,EC 50 介于 200 至 400 pM 之间。GLK-33 包含人源化抗 CD33 抗体 Lintuzumab (HY-P9983),与药物-连接子偶联物 mavg-MMAU (HY-185154) 构成。GLK-33 表现出靶向特异性的抗体依赖性细胞毒性活性。GLK-33 能够降低 CD33 阳性白血病细胞及多药耐药细胞的活力和补体依赖性细胞毒作用 (CDC) 活性。GLK-33 在体内显示出抗肿瘤活性。GLK-33 可用于急性髓系白血病 (AML) 的相关研究。

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GLK-33

GLK-33 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

GLK-33 is a CD33+ antibody-drug conjugate (ADC). GLK-33 binds to human CD33 with an EC 50 value between 200 and 400 pM. GLK-33 consists of the humanized anti-CD33 antibody Lintuzumab (HY-P9983), and the drug-linker conjugate being mavg-MMAU (HY-185154). GLK-33 shows target-specific antibody-dependent cellular cytotoxicity (ADCC) activity and complement-dependent cytotoxicity (CDC) activity against CD33-positive leukemia cell lines. GLK-33 reduces cell viability within CD33-positive leukemia and multidrug-resistant cells. GLK-33 demonstrates antitumor activity in vivo. GLK-33 can be used for acute myeloid leukemia (AML) research[1].

反应种属

Human

IC50 & Target

Siglec-3/CD33

体外研究
(In Vitro)

GLK-33 (0-24小时) 可结合并被 CD33+ 白血病细胞内化[1]
GLK-33 不结合猴或小鼠的CD33-Fc融合蛋白[1]
GLK-33 (1-10000 ng/mL,3-5 天) 对 CD33+ 白血病细胞系及多重耐药细胞系显示出靶向特异性的细胞毒活性[1]
GLK-33 (0.1-10000 nM,30 分钟) 在 MOLM-13 与 NK 细胞共培养体系中显示出靶向特异性的 ADCC 活性,其 EC50 为5 nM[1]
GLK-33 (1-10 µg/mL,0-24 小时) 在 HL-60 细胞中保留了 Fc 受体依赖性的 ADCC 及 CDC 免疫效应功能[1]
GLK-33 (0.001-1000 nM,3-5天) 与 HL-60 细胞表面 CD33 的结合高度稳定,且不易受可溶性靶抗原的干扰[1]
GLK-33 (5 天) 能有效靶向患者单个核细胞中的原始细胞,中位 IC50 值为 16 nM,且无脱靶淋巴细胞毒性[1]

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

Cell Viability Assay[1]

Cell Line: MV4-11, MOLM-13, HL-60, KG-1, OCI-M1, K-562, Daudi and Ramos cells
Concentration: 1, 10, 100, 1000 and 10000 ng/mL
Incubation Time: 3-5 days
Result: Exerted cytotoxicity against MV4-11, MOLM-13, HL-60, KG-1, OCI-M1 and K-562 cells with IC50 values of 0.14, 0.21, 0.24, 1.4, 2.7 and 725 nM, respectively.
Had no cytotoxicity to CD33-negative Daudi lymphoma cells (including Daudi and Ramos cells).
Inhibited KG-1 cells 3-fold more effectively in the presence of Verapamil (HY-14275).
体内研究
(In Vivo)

GLK-33 (300 µg/kg-3 mg/kg,单次静脉注射) 在皮下 HL-60 异种移植瘤小鼠模型中显示出高效的抗白血病活性[1]
GLK-33 (100 µg/kg-1 mg/kg,单次静脉注射) 在皮下 MOLM-13 异种移植瘤中显示出靶向特异性的抗白血病肿瘤活性[1]

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

Animal Model: HL-60 cells (2 x 104, s.c.) induced-Rj:ATHYMIC-Foxn1 nu/nu female mice (8 weeks, 17-23g)[1]
Dosage: 300 µg/kg, 1 mg/kg, 3 mg/kg
Administration: i.v., once
Result: Led to the disappearance of HL-60 xenograft tumors in all mice (100% complete responses, CR) at 3 mg/kg.
Removed the tumors in all mice (100% CR) at 1 mg/kg.
Significantly inhibited tumor growth at 300 µg/kg.
Animal Model: MOLM-13 cells (2 x 104, s.c.) induced-Rj:ATHYMIC-Foxn1nu/nu female mice (8 weeks, 17-23g)[1]
Dosage: 100 µg/kg, 300 µg/kg, 1 mg/kg, 3 mg/kg
Administration: i.v., once
Result: Eradicated the tumors in all mice (100% CR).
Showed dose-dependent activity at 100 µg/kg, 300 µg/kg, 1 mg/kg.
Inhibited tumor growth down to 300 mg/kg.
基因 ID

945  [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:
GLK-33
目录号:
HY-P991910
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