Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-
- Product Name
- Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-
- CAS No.
- 2201056-66-6
- Chemical Name
- Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-
- Synonyms
- S-095033;AG-270 (AG270);AG-270, 10 mM in DMSO;Intermediate material 100102;inhibit,Inhibitor,cancer,Low,solid,AG-270,SAM,pancreatic,lymphoma,tumor,AG 270,toxicity,AG270;3-(1-Cyclohexenyl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one;3-(Cyclohex-1-en-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(pyridin-2-ylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one;Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-;Pyrazolo[1,5-a]pyrimidin-7(4H)-one,?3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)- Pyrazolo[1,5-a]pyrimidin-7(4H)-one,?3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-
- CBNumber
- CB58370861
- Molecular Formula
- C30H27N5O2
- Formula Weight
- 489.57
- MOL File
- 2201056-66-6.mol
Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)- Property
- Boiling point:
- 709.3±70.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- solubility
- DMSO: Slightly soluble
- form
- A solid
- pka
- 7.30±0.10(Predicted)
- color
- White to off-white
- InChIKey
- HSVRUECLQUGTDS-UHFFFAOYSA-N
- SMILES
- C12=C(C3CCCCC=3)C(C3=CC=CC=C3)=NN1C(=O)C(C1=CC=C(OC)C=C1)=C(NC1=NC=CC=C1)N2
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H314Causes severe skin burns and eye damage
- Precautionary statements
-
P260Do not breathe dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301+P330+P331IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P310Immediately call a POISON CENTER or doctor/physician.
P321Specific treatment (see … on this label).
P363Wash contaminated clothing before reuse.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- DC12499
- Product name
- AG-270
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- DC12499
- Product name
- AG-270
- Purity
- >98%
- Packaging
- 1g
- Price
- $2600
- Updated
- 2021/12/16
Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)- Chemical Properties,Usage,Production
Uses
AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM[1].
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].
| 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). |
References
[1] Zenon Konteatis, et al. 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 8. DOI:10.1021/acs.jmedchem.0c01895
[2] Marc L Hyer, et al. The MAT2A inhibitor AG-270 combines with both taxanes and gemcitabine to yield enhanced antitumor activity in patient-derived xenograft models.
Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)- Preparation Products And Raw materials
Raw materials
Preparation Products
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