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Product details

名称

AG-270

分子类型

未知

英文别名

BDBM50576021 | UNII-E1P2TDU69L | NSC835817 | NSC-835817 | 3-Cyclohexenyl-6-(4-methoxyphenyl)-2-phenyl-5-(pyridin-2-ylamino)pyrazolo[1,5-a]pyrimidin-7(4H)-one | AT37360 | HY-138630 | MFCD34368529 | 3-(cyclohex-1-en-1-yl)-6-(4-methoxyphenyl)-2-phenyl-5-[(py

英文名称

AG-270

货号

A648759-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC 50 of 14 nM In Vitro AG-270 demonstrates potent reduction in levels of intracellular SAM , as well as MTAP-–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro. AG-270 exhibits an IC 50 of 20 nM in HCT116 MTAP- cell SAM at 72 h. MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . 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- xenografts and is well tolerated, with mean body weight loss Form:Solid IC50& Target:IC50: 14 nM (MAT2A)

生化机理

AG-270 是一种异构、非竞争性、一流、可逆和口服活性 MAT2A 抑制剂，其 IC 50 为 14 nM。

CAS号

2201056-66-6

分子式

C30H27N5O2

分子量

489.57 g/mol

PubChem编号

134307820

Isomeric SMILES

COC1=CC=C(C=C1)C2=C(N=C3C(=C(NN3C2=O)C4=CC=CC=C4)C5=CCCCC5)NC6=CC=CC=N6

IIUPAC Name

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

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/h3,6-10,12-19,34H,2,4-5,11H2,1H3,(H,31,32)

InChi Key

LSOYYWKBUKXUHQ-UHFFFAOYSA-N

Smiles

COC1=CC=C(C=C1)C2=C(N=C3C(=C(NN3C2=O)C4=CC=CC=C4)C5=CCCCC5)NC6=CC=CC=N6

PubChem CID

134307820

关联CAS

2201056-66-6

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

489.216 Da

单同位素质量Monoisotopic Mass

489.216 Da

拓扑极表面积Topological Polar Surface Area

78.900 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

997.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

5.600

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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