|(S)-2-((S)-2-苄基-4-((5-甲基-1H-咪唑-4-基)甲基)-3-氧代哌嗪-1-甲酰胺基)-4-甲基戊酸|CsnPharm

CAS No.: 501010-06-6

GGTI-2418 Catalog No. CSN23732

Synonyms: PTX-100

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1].

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The ability of the GTPases to mediate these tumorigenic events requires their posttranslational modification with farnesyl and geranylgeranyl lipids. The enzymes responsible for these modifications is geranylgeranyltransferase I (GGTI), and inhibitors of GGTI have been developed as potential anticancer drugs. GGTI-2418 is a potent and selective peptidomimetic inhibitor of GGTI. In vitro, GGTI-2418 inhibits GGTI with IC₅₀ of 9.5 ± 2.0 nM. And it demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a K_i value of 4.4 ± 1.6 nM. Tumors from mice treated with 100 mg/kg GGTI-2418 intraperitoneally daily or 200 mg/kg every third day grew to only average tumor sizes of 139 ± 17 or 276 ± 26 mm³, respectively, corresponding to tumor growth inhibitions of 94% and 77%, respectively (P < 0.005 for both). These data clearly indicate that GGTI-2418 potently inhibits the growth of breast tumor xenografts with either daily or intermittent dosing. Moreover, in seven mice with a total of 17 tumors, treatment with 100 mg/kg GGTI-2418 resulted in tumor regression between 34 and 100%, with an average of 60% ± 4%^[1].
参考文献

[1] Kazi A, Carie A, Blaskovich MA, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009;29(8):2254‐2263

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2649 mL
- 11.3244 mL
- 22.6489 mL
- 5 mM
- 0.4530 mL
- 2.2649 mL
- 4.5298 mL
- 10 mM
- 0.2265 mL
- 1.1324 mL
- 2.2649 mL

技术信息

CAS号

501010-06-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H31N5O4

运输

蓝冰

分子量

441.52

别名

PTX-100

溶解度

DMSO	31.33 mg/mL (71.0 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

GGTI-2418 Catalog No. CSN23732

靶点选择性

请登录您的专属账户

确认信息