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Chemical Structure| 1419949-20-4 Chemical Structure| 1419949-20-4

Structure of NVP-TNKS656
CAS No.: 1419949-20-4

Chemical Structure| 1419949-20-4

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NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, showing > 300 fold selectivity against PARP1 and PARP2.

Synonyms: TNKS656

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Product Details of NVP-TNKS656

CAS No. :1419949-20-4
Formula : C27H34N4O5
M.W : 494.58
SMILES Code : O=C(N(CC1CC1)CC2=NC3=C(COCC3)C(N2)=O)CN4CCC(C(C5=CC=C(OC)C=C5)=O)CC4
Synonyms :
TNKS656
MDL No. :MFCD28167762
InChI Key :DYGBNAYFDZEYBA-UHFFFAOYSA-N
Pubchem ID :136237316

Safety of NVP-TNKS656

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of NVP-TNKS656

epigenetics
DNA

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MHCC-97h 1.25 to 100 μM 3 days NVP-TNKS656 inhibited the proliferation of MHCC-97h cells in a dose-dependent manner. PMC10691066
SMMC-7721 1.25 to 100 μM 3 days NVP-TNKS656 inhibited the proliferation of SMMC-7721 cells in a dose-dependent manner. PMC10691066
MHCC-97h 1.25 to 100 μM 3 days NVP-TNKS656 inhibited the proliferation of MHCC-97h cells in a dose-dependent manner. PMC6930431
SMMC-7721 1.25 to 100 μM 3 days NVP-TNKS656 inhibited the proliferation of SMMC-7721 cells in a dose-dependent manner. PMC6930431
HCT116 isogenic cell lines (54, 240, 241) 5 μM 48 hours To evaluate the effect of NVP-TNKS656 combined with MEK inhibitor on colon cancer cells with different β-catenin genotypes. Results showed that β-catenin wild-type cells (241) responded to the combination treatment, while mutant (240) and mixed (54) cells did not. PMC6734664
HCT-8 5 μM 48 hours To evaluate the effect of NVP-TNKS656 combined with MEK inhibitor on PIK3CA mutant colon cancer cells. Results showed that the combination treatment significantly increased cell death. PMC6734664
DLD-1 5 μM 48 hours To evaluate the effect of NVP-TNKS656 combined with MEK inhibitor on PIK3CA mutant colon cancer cells. Results showed that the combination treatment significantly increased cell death. PMC6734664

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice DLD-1 PIK3CA mt (cell line 353) xenograft model Intraperitoneal injection 50 mg/kg Once daily for 28 days To evaluate the effect of NVP-TNKS656 combined with MEK inhibitor on PIK3CA mutant colon cancer Mice model. Results showed that the combination treatment significantly suppressed tumor growth. PMC6734664

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.11mL

2.02mL

1.01mL

20.22mL

4.04mL

2.02mL

References

 

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