2. Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt
  3. PARP Wnt β-catenin
  4. G-631

G-631 是一种具有口服活性的 tankyrase (TNKS1/TNKS2) 抑制剂。G-631 可稳定 AXIN、抑制 Wnt/β-catenin 信号通路。G-631 在结直肠癌小鼠模型中表现出微弱的抗肿瘤活性。G-631 可用于结直肠癌等癌症的相关研究。

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G-631

G-631 Chemical Structure

CAS No. : 1507370-78-6

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规格 价格 是否有货 数量
1 mg ￥1394
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5 mg ￥3485
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10 mg ￥5576
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G-631 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

G-631 is an orally active tankyrase(TNKS1/TNKS2) inhibitor. G-631 stabilizes AXIN and inhibits the Wnt/β-catenin signaling pathway. G-631 exhibits weak anti-tumor activity in mouse models of colorectal cancer. G-631 can be used in studies related to cancers such as colorectal cancer[1].

体外研究
(In Vitro)

G-631 是一种强效且选择性的 TNKS1/2 抑制剂，在 HEK293 细胞中的生化 IC50 为 7 nM，细胞水平 IC50 为 8 nM[1]。
G-631 (10 μM) 对人去甲肾上腺素转运体表现出 56% 的结合抑制活性[1]。

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

G-631 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-24 Cmax Tmax AUC
Mice[1] 6.5 mg/kg p.o. 25.7 μM·h 7.81 μM 0.5 h 1.66
Mice[1] 12.5 mg/kg p.o. 54.1 μM·h 11.7 μM 0.5 h 1.82
Mice[1] 25 mg/kg p.o. 52.8 μM·h 21.4 μM 0.5 h 0.887
Mice[1] 50 mg/kg p.o. 83.2 μM·h 20.7 μM 0.5 h 0.699
Mice[1] 100 mg/kg p.o. 114 μM·h 40.3 μM 0.5 h 0.479
Mice[1] 25 mg/kg p.o. / 7.4 μM 1.0 h /
Mice[1] 25 mg/kg p.o. / 6.8 μM 1.0 h /
Mice[1] 100 mg/kg p.o. / 23.4 μM 1.0 h /
Mice[1] 100 mg/kg p.o. / 13.9 μM 1.0 h /
体内研究
(In Vivo)

G-631 (6.25-100 mg/kg；灌胃；每日 1 次/2 次；21 天) 在 SW403 结直肠癌异种移植模型中呈剂量依赖性抑制 Wnt/β-catenin 信号通路[1]。

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

Animal Model: nu/nu mice (female, 6-8 weeks of age, implanted with SW403 colorectal adenocarcinoma cells)[1]
Dosage: 6.25-100 mg/kg; 25 mg/kg (twice daily, not tolerated); 50 mg/kg (twice daily, not tolerated); 100 mg/kg (once daily, MTD)
Administration: p.o.; once daily; 21 days; p.o.; twice daily; 21 days
Result: Caused a dose-dependent reduction in relative TNFRSF19 mRNA levels in tumors.
Reduced mean tumor volume.
Induced approximately 10% body weight loss at 100 mg/kg once daily.
Was not tolerated at 25 and 50 mg/kg twice daily, with greater than 10% body weight loss.
分子量

420.41

Formula

C19H22F2N6O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

G-631 相关分类

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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.

Keywords:

G-6311507370-78-6G631G 631PARPWntβ-cateninpoly ADP ribose polymerase Beta cateninWnt/β-catenin signalingAXINHEK293 cellsSW403 colorectal cancer xenograftsnu/nu miceInhibitorinhibitorinhibit

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