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MedKoo Cat#: 207026 | Name: AG-270 HCl
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Description:

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

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
AG-270 HCl
CAS#13299-99-5 (HCl)

Theoretical Analysis

MedKoo Cat#: 207026

Name: AG-270 HCl

CAS#: 13299-99-5 (HCl)

Chemical Formula: C18H24ClN3O3

Exact Mass: 0.0000

Molecular Weight: 365.86

Elemental Analysis: C, 59.09; H, 6.61; Cl, 9.69; N, 11.49; O, 13.12

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 weeks
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Related CAS #
2201056-66-6 (free base) 2761546-65-8 (sodium) 13299-99-5 (HCl)
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/
Solvent mg/mL mM comments
Solubility
Soluble in DMSO 0.0 0.00
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 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.

Recalculate based on batch purity %
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
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.