K-756 | CAS#130017-40-2 | Wnt/β-catenin pathway inhibitor

MedKoo Cat#: 558248 | Name: K-756

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

K-756 is a a selective Wnt/β-catenin pathway inhibitor. K-756 is also a tankyrase (TNKS) inhibitor. K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. could be a leading compound in the development of anticancer agents.

Chemical Structure

K-756

CAS#130017-40-2

Theoretical Analysis

MedKoo Cat#: 558248

Name: K-756

CAS#: 130017-40-2

Chemical Formula: C24H27N5O3

Exact Mass: 433.2114

Molecular Weight: 433.51

Elemental Analysis: C, 66.50; H, 6.28; N, 16.16; O, 11.07

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 Weeks
10mg	USD 700.00	2 Weeks

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Related CAS #

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Synonym

K-756; K 756; K756;

IUPAC/Chemical Name

3-[1-(6,7-Dimethoxy-quinazolin-4-yl)-piperidin-4-ylmethyl]-3,4-dihydro-1H-quinazolin-2-one

InChi Key

GWXCGEJJQFHPPA-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H27N5O3/c1-31-21-11-18-20(12-22(21)32-2)25-15-26-23(18)28-9-7-16(8-10-28)13-29-14-17-5-3-4-6-19(17)27-24(29)30/h3-6,11-12,15-16H,7-10,13-14H2,1-2H3,(H,27,30)

SMILES Code

O=C1NC2=C(C=CC=C2)CN1CC3CCN(C4=C5C=C(OC)C(OC)=CC5=NC=N4)CC3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TMS1 amd TMLS2 with IC50s of 31 and 36 nM, respectively.

In vitro activity:

K-756 binds to the induced pocket of TNKS and inhibits its enzyme activity. Moreover, PARP family enzyme assays showed that K-756 is a selective TNKS inhibitor. K-756 inhibited the cell growth of APC-mutant colorectal cancer COLO 320DM and SW403 cells by inhibiting the Wnt/β-catenin pathway. Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/

In vivo activity:

An in vivo study showed that the oral administration of K-756 inhibited the Wnt/β-catenin pathway in colon cancer xenografts in mice. Reference: Mol Cancer Ther. 2016 Jul;15(7):1525-34. https://pubmed.ncbi.nlm.nih.gov/27196752/

	Solvent	mg/mL	mM
Solubility
	DMSO	4.6	10.50

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 433.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Okada-Iwasaki R, Takahashi Y, Watanabe Y, Ishida H, Saito J, Nakai R, Asai A. The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase. Mol Cancer Ther. 2016 Jul;15(7):1525-34. doi: 10.1158/1535-7163.MCT-15-0938. Epub 2016 Apr 25. PMID: 27196752.

In vitro protocol:

In vivo protocol:

1: Okada-Iwasaki R, Takahashi Y, Watanabe Y, Ishida H, Saito J, Nakai R, Asai A. The Discovery and Characterization of K-756, a Novel Wnt/β-Catenin Pathway Inhibitor Targeting Tankyrase. Mol Cancer Ther. 2016 Jul;15(7):1525-34. doi: 10.1158/1535-7163.MCT-15-0938. Epub 2016 Apr 25. PubMed PMID: 27196752.