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

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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

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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..…

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N-Bromosuccinimide Price

DC Chemicals

Product number: DC12499
Product name: AG-270
Purity: >98%
Packaging: 250mg
Price: $1500
Updated: 2021/12/16

DC Chemicals

Product number: DC12499
Product name: AG-270
Purity: >98%
Packaging: 1g
Price: $2600
Updated: 2021/12/16

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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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Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)- Suppliers

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2201056-66-6, Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-Related Search:

Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(1-cyclohexen-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridinylamino)-

3-(1-Cyclohexenyl)-6-(4-methoxyphenyl)-2-phenyl-5-(2-pyridylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one

AG-270 (AG270)

inhibit,Inhibitor,cancer,Low,solid,AG-270,SAM,pancreatic,lymphoma,tumor,AG 270,toxicity,AG270

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)-

AG-270, 10 mM in DMSO

S-095033

Intermediate material 100102

2201056-66-6