AZ6102 | CAS#1645286-75-4 | TNKS1/2 inhibitor

AZ6102
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407211

CAS#: 1645286-75-4

Description: AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. AZ6102 can be formulated well in a clinically relevant intravenous solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclinical species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ß-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin.

Chemical Structure

AZ6102

CAS# 1645286-75-4

Instruction

Theoretical Analysis

MedKoo Cat#: 407211
Name: AZ6102
CAS#: 1645286-75-4
Chemical Formula: C25H28N6O
Exact Mass: 428.23
Molecular Weight: 428.540
Elemental Analysis: C, 70.07; H, 6.59; N, 19.61; O, 3.73

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1350	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 4250	2 Weeks
2g	USD 6850	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: AZ6102; AZ-6102; AZ 6102.

IUPAC/Chemical Name: 2-(4-(6-((3R,5S)-3,5-dimethylpiperazin-1-yl)-4-methylpyridin-3-yl)phenyl)-7-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one

InChi Key: WCPTUQOMNJBIET-CALCHBBNSA-N

InChi Code: InChI=1S/C25H28N6O/c1-15-11-22(31-13-16(2)27-17(3)14-31)26-12-21(15)18-5-7-19(8-6-18)23-28-24-20(25(32)29-23)9-10-30(24)4/h5-12,16-17,27H,13-14H2,1-4H3,(H,28,29,32)/t16-,17+

SMILES Code: O=C1C2=C(N(C)C=C2)N=C(C3=CC=C(C4=C(C)C=C(N5C[C@@H](C)N[C@@H](C)C5)N=C4)C=C3)N1

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, not in water

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 428.54 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:
In vitro protocol:
In vivo protocol:

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1: Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA,
Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J,
Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG,
Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T.
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway
inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett. 2015 Jan
13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12. PubMed PMID:
25815142; PubMed Central PMCID: PMC4360163.

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AZ6102 featured