2. Antibody-drug Conjugate/ADC Related Protein Tyrosine Kinase/RTK
  3. Antibody-Drug Conjugates (ADCs) FGFR
  4. Aprutumab ixadotin

Aprutumab ixadotin  (Synonyms: BAY 1187982)

目录号: HY-141600

摩尔计算器

Aprutumab ixadotin (BAY 1187982) 是首个靶向 FGFR2 的抗体药物偶联物 (ADC)，也是首个使用奥耳他汀基有效载荷的抗体药物偶联物。

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Aprutumab ixadotin Chemical Structure

Aprutumab ixadotin Chemical Structure

CAS No. : 1708947-48-1

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Aprutumab ixadotin 相关抗体

Top Publications Citing Use of Products

查看 FGFR 亚型特异性产品:

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload[1][2].

体外研究
(In Vitro)

Aprutumab ixadotin (0.097-0.83 nM; 72 h) 对 FGFR2 表现出 0.29 nM 的抗原结合亲和力，并在几个癌细胞系中表现出抑制活性，IC50 为 0.097-0.83 nM[1]。
Aprutumab ixadotin 还诱导 FGFR2 阳性细胞凋亡 (SUN-52PE, SUN-16)[1]。

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

Aprutumab ixadotin 相关抗体:

Cell Viability Assay[1]

Cell Line: SNU-16, KATO III, SUM-52PE, NCI-H716, and MFM-223 cells; MDA-MB-231 cells; KYSE-180 cells; 4T1 cells
Concentration: 0.097-0.83 nM
Incubation Time: 72 hours
Result: Inhibited cell viability.
体内研究
(In Vivo)

Aprutumab ixadotin (5 mg/kg 或 7.5 mg/kg; 静脉注射; 每周一次, 共 30 天) 耐受性良好，可导致小鼠中 SNU-16、MFM-223 或 NCI-H716 异种移植物模型肿瘤部分消退[1]。

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

Animal Model: SNU-16 xenograft model in female NOD scid mice and MFM-223 and NCI-H716 xenograft models in female NMRI nu/nu mice[1]
Dosage: 0.5 mg/kg, 1 mg/kg, 5 mg/kg, 7.5 mg/kg, 15 mg/kg
Administration: Intravenous injection; once weekly for 4 weeks
Result: Significantly tumor growth at least 90% at 5 mg/kg in SNU-16 xenograft model. However, doses of 0.5 or 1 mg/kg did not significantly inhibit tumor growth compared to the vehicle control.
Marked decrease in tumor volume at 1 and 5 mg/kg in MFM-223 model.
Resulted in notable inhibition of tumor growth at 7.5 mg/kg in cell line derived xenograft model overexpressing FGFR2, the NCI-H716 human colorectal cancer model.
CAS 号
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

Aprutumab ixadotin 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Aprutumab ixadotin1708947-48-1BAY 1187982BAY1187982BAY-1187982Antibody-Drug Conjugates (ADCs)FGFRAntibody-Drug ConjugatesFibroblast growth factor receptorInhibitorinhibitorinhibit

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目录号：
HY-141600
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