AG-270
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MedKoo CAT#: 464642

CAS#: 2201056-66-6 (free)

Description: AG-270 is a first-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion.

Chemical Structure

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AG-270
CAS# 2201056-66-6 (free)
Instruction

Theoretical Analysis

MedKoo Cat#: 464642
Name: AG-270
CAS#: 2201056-66-6 (free)
Chemical Formula: C30H27N5O2
Exact Mass: 489.22
Molecular Weight: 489.579
Elemental Analysis: C, 73.60; H, 5.56; N, 14.31; O, 6.54

Price and Availability

Size Price Availability Quantity
5mg USD 550 2 Weeks
25mg USD 1650 2 Weeks
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Related CAS #: 2201056-66-6 (free)   2761546-65-8 (sodium)    

Synonym: AG-270; AG270; AG 270;

IUPAC/Chemical Name: 3-(cyclohex-1-en-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(pyridin-2-ylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one

InChi Key: HSVRUECLQUGTDS-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H27N5O2/c1-37-23-17-15-21(16-18-23)26-28(32-24-14-8-9-19-31-24)33-29-25(20-10-4-2-5-11-20)27(34-35(29)30(26)36)22-12-6-3-7-13-22/h3,6-10,12-19,33H,2,4-5,11H2,1H3,(H,31,32)

SMILES Code: O=C1C(C2=CC=C(OC)C=C2)=C(NC3=NC=CC=C3)NC4=C(C5=CCCCC5)C(C6=CC=CC=C6)=NN14

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 489.58 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
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.