1. Protein Tyrosine Kinase/RTK MAPK/ERK Pathway JAK/STAT Signaling Stem Cell/Wnt PI3K/Akt/mTOR
  2. FLT3 p38 MAPK STAT PI3K Akt
  3. IMC-EB10

IMC-EB10  (Synonyms: LY3012218)

目录号: HY-P991641
技术支持

IMC-EB10 (LY3012218) 是一种抗 FLT3 单克隆抗体。IMC-EB10 能够高亲和力 (Kd = 158 pM) 结合 FLT3,并阻断 FLT3 配体与 FLT3 的结合 (IC50 ≈ 10 nM),进而抑制白血病细胞中的 MAPKSTAT5PI3K/Akt 信号传导。IMC-EB10 可以增强 Methotrexate (HY-14519) 抗白血病的效果,抑制表达野生型或 ITD 突变型 FLT3 受体的白血病。IMC-EB10 延长急性淋巴细胞白血病 (ALL) 细胞系和原发性白血病样本的生存期并减少非肥胖糖尿病/严重联合免疫缺陷的植入。IMC-EB10 可用于白血病研究。

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IMC-EB10

IMC-EB10 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research[1][2][3][4].

同型

Human IgG1 kappa

推荐同型对照抗体
反应种属

Human

IC50 & Target[1][4]

STAT5

 

体外研究
(In Vitro)

IMC-EB10 (10 μg/mL,1 小时) 可降低 Hb1119 和 SEM-K2 细胞中的 FLT3 及其下游信号蛋白 STAT5、Akt 和 MAPK 的磷酸化,但在 REH 和 RS411 细胞中可激活这些蛋白[1]
IMC-EB10 (10 μg/mL,1 小时) 可激活 ALLs 中的 FLT3 及其下游 Akt[1]
IMC-EB10 (0.4-200 nM,1 小时) 可抑制 EOL-1、EM3、BaF3-ITD 和 MV4;11 细胞中 FLT3-Fc 诱导的野生型 FLT3 磷酸化以及 ITD 突变体 FLT3 的配体非依赖性组成性磷酸化[4]
IMC-EB10 (0.4-200 nM,1 小时) 可抑制 FLT3-Fc 诱导的 EOL-1、EM3、BaF3-ITD 和 MV4;11 细胞中 MAPK、AKT 和 Stat5 磷酸化[4]
IMC-EB10 (1.5-100 nM,1 小时) 可抑制 FLT3-Fc 诱导的 EOL-1 和 BaF3-ITD 细胞增殖[4]

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

Western Blot Analysis[1]

Cell Line: Hb1119, SEM-K2 cells
Concentration: 10 μg/mL
Incubation Time: 1 h
Result: Reduced FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK.

Western Blot Analysis[1]

Cell Line: REH, RS411 cells
Concentration: 10 μg/mL
Incubation Time: 1 h
Result: Activated FLT3 and phosphorylation of downstream signaling proteins STAT5, Akt, and MAPK.

Western Blot Analysis[1]

Cell Line: ALLs
Concentration: 10 μg/mL
Incubation Time: 1 h
Result: Activated FLT3 and downstream Akt.

ELISA Assay[4]

Cell Line: EOL-1, EM3, BaF3-ITD, MV4;11 cells
Concentration: 0.1, 0.4, 1, 4, 10, 40, 100, 200 nM
Incubation Time: 1 h
Result: Blocked FL-induced FLT3 receptor phosphorylation in a dose dependent manner with an IC50 of 0.4 to 4 nM.
Blocked the phosphorylation and constitutive phosphorylation of MAPK, inhibited FL-induced phosphorylation of AKT and Stat5 phosphorylation in EOL-1 and BaF3-ITD cells.
体内研究
(In Vivo)

IMC-EB10 (400 μg/10 mg/kg,腹腔注射,细胞注射后 24 小时开始每周三次/细胞注射后 24 小时开始一次/细胞注射后 24 小时开始每隔一天共三次或细胞注射后 7 天开始每周三次,共 30 天/每周 2 次,共 3 周) 在 SEM-K2 NOD/SCID 小鼠模型中可减少 SEM-K2 细胞的存在,通过自然杀伤细胞介导细胞毒性,不会选择耐药细胞,与单独使用 Methotrexate (HY-14519) 相比可延长生存期[1][3]
IMC-EB10 (400 μg,腹腔注射,每周三次,共 14 周) 可减少 ALLs NOD/SCID 小鼠模型中的细胞植入[1]
IMC-EB10 (100-500 μg,腹腔注射,每周 3 次,共 20 天) 在 EOL-1 和 BaF3-ITD 异种移植白血病模型中可减少骨髓中的肿瘤细胞数量,并延长生存期[4]

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

Animal Model: SEM-K2 (0.5×106) NOD/SCID mice model[1]
Dosage: 400 μg
Administration: i.p., thrice per week starting 24 hours after cell injection/once starting 24 hours after cell injection/a total of thrice every other day starting 24 hours after cell injection or thrice per week starting 7 days after cell injection, 30 days
Result: Reduced human cells in peripheral blood, spleen, and bone marrow, reducing the presence of SEM-K2 cells to <1%, prolonged survival. Did not select for resistant cells, mediated cytotoxicity through natural killer cells.
Animal Model: ALLs (1×106) NOD/SCID mice model[1]
Dosage: 400 μg
Administration: i.p., three times a week, 14 weeks
Result: Reduced cell implantation.
Animal Model: SEM-K2 (5×105) NOD/SCID mice model[3]
Dosage: 10 mg/kg + 100 mg/kg Methotrexate
Administration: i.p., 2×/week, 3 weeks + once per week for 3 weeks
Result: Significantly prolonged survival compared to Methotrexate alone.
Animal Model: EOL-1 (5×106) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4]
Dosage: 100, 250, 500 μg
Administration: i.p., 3 times weekly, 20 days
Result: Decreased the number of tumor cells in bone marrow.
Animal Model: BaF3-ITD (5×104) xenograft leukemia NOD/SCID mice (male, , 6-8 weeks) model[4]
Dosage: 100, 500 μg
Administration: i.p., 3 times weekly
Result: Prolonged the survival.
基因 ID

2322  [NCBI]

Accession
靶点

FLT3

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
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  • 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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IMC-EB10
目录号:
HY-P991641
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