1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. GGTI-297

GGTI-297 是一种香叶基香叶基转移酶 I (GGTase-1) 抑制剂,对 GGTase-1 和法呢基转移酶 (FTase) 的 IC50 值分别为 56 nM 和 203 nM。GGTI-297 抑制香叶基香叶基化蛋白 Rap1A 的加工,而不影响法呢基化蛋白 H-Ras

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GGTI-297 Chemical Structure

GGTI-297 Chemical Structure

CAS No. : 181045-83-0

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生物活性

GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC50 values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras[1][2].

体内研究
(In Vivo)

GGTI-297(70 mg/kg;腹腔注射;每天一次;持续 5-7 周)可抑制裸鼠中 A-549 和 Calu-1 异种移植瘤的生长,这两种移植瘤均表达 K-Ras 突变[2]

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

Animal Model: Nude mice injected (8 week old) with A-549 or Calu-1 cells[2]
Dosage: 70 mg/kg
Administration: ip; once a day; for 5 weeks (A-549 cells) and 12 weeks (Calu-1)
Result: Inhibited the growth in nude mice of A-549 and Calu-1 xenografts.
分子量

465.61

Formula

C26H31N3O3S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

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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  • 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:
GGTI-297
目录号:
HY-120271
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