AG-270 HCl| CAS#13299-99-5 | MAT2A inhibitor

AG-270 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 207026

CAS#: 13299-99-5 (HCl)

Description: AG-270 is a potent and orally active MAT2A inhibitor with potential antineoplastic activity. AG-270 inhibits the activity of MAT2A, a metabolic enzyme responsible for the production of S-Adenosyl-L-methionine (SAM), a primary donor of methyl groups in cellular transmethylation reactions that regulate gene expression, cell growth, and differentiation.

Chemical Structure

AG-270 HCl

CAS# 13299-99-5 (HCl)

Instruction

Theoretical Analysis

MedKoo Cat#: 207026
Name: AG-270 HCl
CAS#: 13299-99-5 (HCl)
Chemical Formula: C18H24ClN3O3
Exact Mass: 0.00
Molecular Weight: 365.858
Elemental Analysis: C, 59.09; H, 6.61; Cl, 9.69; N, 11.49; O, 13.12

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450
100mg	USD 1250
200mg	USD 1950
500mg	USD 2950
1g	USD 3950
2g	USD 6450
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.

Related CAS #: 13299-99-5 (HCl) 13299-98-4 (free base)

Synonym: RUN99995; RUN-99995; RUN 99995; MAT2A inhibitor 2; AG-270; AG 270; AG270; AG-270 HCl; AG-270 hydrochloride

IUPAC/Chemical Name: 6-(m-Methoxyphenyl)-4-methyl-2-(2-morpholinoethyl)-3(2H)-pyridazinone hydrochloride

InChi Key: REOUTEBTFSILJY-UHFFFAOYSA-N

InChi Code: InChI=1S/C18H23N3O3.ClH/c1-14-12-17(15-4-3-5-16(13-15)23-2)19-21(18(14)22)7-6-20-8-10-24-11-9-20;/h3-5,12-13H,6-11H2,1-2H3;1H

SMILES Code: O=C1C(C)=CC(C2=CC=CC(OC)=C2)=NN1CCN3CCOCC3.[H]Cl

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: >3 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: MAT2A activity is selectively essential in cancer cells deficient in methylthioadenosine phosphorylase (MTAP), a critical enzyme in the methionine salvage pathway, that is deleted in some human cancers. Inhibition of MAT2A may potentially inhibit tumor cell growth in MTAP-deleted cancers that rely heavily on SAM synthesis. For hodoodo-chemical-nomenclature: https://hodoodo.com/hodoodo-chemical-nomenclature/

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	Soluble in DMSO	0.0	0.00

Preparing Stock Solutions

The following data is based on the product molecular weight 365.86 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: Konteatis Z, Travins J, Gross S, Marjon K, Barnett A, Mandley E, Nicolay B, Nagaraja R, Chen Y, Sun Y, Liu Z, Yu J, Ye Z, Jiang F, Wei W, Fang C, Gao Y, Kalev P, Hyer ML, DeLaBarre B, Jin L, Padyana AK, Dang L, Murtie J, Biller SA, Sui Z, Marks KM. Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion. J Med Chem. 2021 Apr 22;64(8):4430-4449. doi: 10.1021/acs.jmedchem.0c01895. Epub 2021 Apr 8. PMID: 33829783.

2: Kalev P, Hyer ML, Gross S, Konteatis Z, Chen CC, Fletcher M, Lein M, Aguado- Fraile E, Frank V, Barnett A, Mandley E, Goldford J, Chen Y, Sellers K, Hayes S, Lizotte K, Quang P, Tuncay Y, Clasquin M, Peters R, Weier J, Simone E, Murtie J, Liu W, Nagaraja R, Dang L, Sui Z, Biller SA, Travins J, Marks KM, Marjon K. MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. doi: 10.1016/j.ccell.2020.12.010. Epub 2021 Jan 14. PMID: 33450196.

3: Guo J, Yang Y, Buettner R, Rosen ST. Targeting the methionine-methionine adenosyl transferase 2A- S -adenosyl methionine axis for cancer therapy. Curr Opin Oncol. 2022 Sep 1;34(5):546-551. doi: 10.1097/CCO.0000000000000870. Epub 2022 Jul 5. PMID: 35788128; PMCID: PMC9365249.

4: Kang H, Guo Q, Dong Y, Peng R, Song K, Wang J, Liu H, Zhu M, Zhao H, Guan H, Li F. Inhibition of MAT2A suppresses osteoclastogenesis and prevents ovariectomy-induced bone loss. FASEB J. 2022 Feb;36(2):e22167. doi: 10.1096/fj.202101205RR. Erratum in: FASEB J. 2023 Mar;37(3):e22755. PMID: 35064691.

5: Kimura Y, Watanabe K, Okuda H. Effects of soluble sodium alginate on cholesterol excretion and glucose tolerance in rats. J Ethnopharmacol. 1996 Oct;54(1):47-54. doi: 10.1016/0378-8741(96)01449-3. PMID: 8941868.

6: Li M, Konteatis Z, Nagaraja N, Chen Y, Zhou S, Ma G, Gross S, Marjon K, Hyer ML, Mandley E, Lein M, Padyana AK, Jin L, Tong S, Peters R, Murtie J, Travins J, Medeiros M, Liu P, Frank V, Judd ET, Biller SA, Marks KM, Sui Z, Reznik SK. Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads. J Med Chem. 2022 Mar 24;65(6):4600-4615. doi: 10.1021/acs.jmedchem.1c01595. Epub 2022 Mar 16. PMID: 35293760.

7: Zhang S, Qing L, Wang Z, Zhang Y, Li Y, Fang H, Liu Y, He H. Design and Structural Optimization of Methionine Adenosyltransferase 2A (MAT2A) Inhibitors with High In Vivo Potency and Oral Bioavailability. J Med Chem. 2023 Apr 13;66(7):4849-4867. doi: 10.1021/acs.jmedchem.2c02006. Epub 2023 Mar 24. PMID: 36961373.

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