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

K-756
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 558248

CAS#: 130017-40-2

Description: 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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 558248
Name: K-756
CAS#: 130017-40-2
Chemical Formula: C24H27N5O3
Exact Mass: 433.21
Molecular Weight: 433.512
Elemental Analysis: C, 66.50; H, 6.28; N, 16.16; O, 11.07

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 600	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	4.6	10.50

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:	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 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. PMID: 27196752.

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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.

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