2. Epigenetics Metabolic Enzyme/Protease
  3. Methionine Adenosyltransferase (MAT)
  4. AG-270

AG-270 

Cat. No.: HY-138630 Purity: 99.58%
COA Handling Instructions

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

For research use only. We do not sell to patients.

AG-270 Chemical Structure

AG-270 Chemical Structure

CAS No. : 2201056-66-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 600 In-stock
25 mg USD 1150 In-stock
50 mg USD 1800 In-stock
100 mg USD 2850 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

AG-270 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AG-270

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM[1].
IC50 & Target

IC50: 14 nM (MAT2A)[1].
In Vitro

AG-270 demonstrates potent reduction in levels of intracellular SAM, as well as MTAP-null–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro[1].
AG-270 exhibits an IC50 of 20 nM in HCT116 MTAP-null cell SAM at 72 h[1].
MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AG-270 Related Antibodies
In Vivo

AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively[1].
AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts and is well tolerated, with mean body weight loss <5%[1].
Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pancreatic KP4 MTAP-null xenograft mouse model[1].
Dosage: 10-200 mg/kg.
Administration: Orally, q.d. for 38 days.
Result: Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).
Clinical Trial
Molecular Weight

489.57

Appearance

Solid

Formula

C30H27N5O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 4 mg/mL (8.17 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0426 mL 10.2130 mL 20.4261 mL
5 mM 0.4085 mL 2.0426 mL 4.0852 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.75 mg/mL (9.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 4.75 mg/mL (9.70 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.72%

COA (254 KB) HNMR (492 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
References
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AG-270 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

AG-2702201056-66-6AG270AG 270Methionine Adenosyltransferase (MAT)S-adenosylmethionine SynthetaseLowtoxicitypancreaticcancerSAMsolidtumorlymphomaInhibitorinhibitorinhibit

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