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

G-631 is an orally active tankyrase(TNKS1/TNKS2) inhibitor. G-631 stabilizes AXIN and inhibits the Wnt/β-catenin signaling pathway. G-631 can be used in studies related to cancers such as colorectal cancer.

For research use only. We do not sell to patients.

G-631

G-631 Chemical Structure

CAS No. : 1507370-78-6

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Based on 1 publication(s) in Google Scholar

G-631 Related Antibodies

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  • Biological Activity

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Description

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

In Vitro

G-631 is a potent and selective TNKS1/2 inhibitor, with a biochemical IC50 of 7 nM and a cellular IC50 of 8 nM in HEK293 cells[1].
G-631 (10 μM) exhibits 56% binding inhibitory activity against the human norepinephrine transporter[1].

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

G-631 Related Antibodies
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 /
In Vivo

G-631 (6.25-100 mg/kg; p.o.; once/twice daily; 21 days) dose-dependently inhibits the Wnt/β-catenin signaling pathway in the SW403 colorectal cancer xenograft model[1].

MedChemExpress (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.
Molecular Weight

420.41

Formula

C19H22F2N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N=C(N2CCN(CC2)C3=C(C=C(C=C3F)OCCOC)F)NC4=C1C=NN4C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (4.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3786 mL 11.8932 mL 23.7863 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3786 mL 11.8932 mL 23.7863 mL 59.4658 mL
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G-631 Related Classifications

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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