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Product details

名称

Pevonedistat hydrochloride

分子类型

小分子

别名

盐酸哌沃地司他

英文别名

MLN-4924-003 | MLN4924-003 | SulfaMic acid [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]aMino]-7H-pyrrolo[2,3-d]pyriMidin-7-yl]-2-hydroxycyclopentyl]Methyl ester hydrochloride | DTXSID70151270 | 1160295-21-5 | MLN 4924 hydrochloride | A927617 | Pevon

英文名称

Pevonedistat hydrochloride

货号

P651845-5mg

包装规格

5mg

浓度

≥99%

储存温度

2-8°C储存,干燥

运输条件

冰袋运输

产品介绍

Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC 50 of 4.7 nM In Vitro Pevonedistat (MLN4924) is a potent inhibitor of NAE (half-maximal inhibitory concentration (IC 50 =0.004 μM), and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC 50 =1.5, 8.2, 1.8 and >10 μM, respectively). Pevonedistat (MLN4924) treatment inhibits overall protein turnover in cultured HCT-116 cells. Treatment of HCT-116 cells with Pevonedistat (MLN4924) for 24 h results in a dose-dependent decrease of Ubc12-NEDD8 thioester and NEDD8-cullin conjugates, with an IC 50 In Vivo Pevonedistat (MLN492410, 30 or 60 mg/kg, s.c.) leads to a dose- and time-dependent increase in the steady state levels of NRF2 and CDT1 in HCT-116 tumour-bearing mice, and decreases NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells. Pevonedistat (MLN4924) administered on a BID schedule at 30 and 60 mg/kg inhibits tumour growth with T/C values of 0.36 and 0.15, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 4.7 nM (NAE)

生化机理

盐酸培伐地司他（MLN4924 盐酸盐）是一种强效、选择性的 NEDD8 激活酶（NAE）抑制剂，IC 50 为 4.7 nM。

CAS号

1160295-21-5

分子式

C21H26ClN5O4S

分子量

480 g/mol

PubChem编号

66576990

Isomeric SMILES

C1CC2=CC=CC=C2[C@H]1NC3=C4C=CN(C4=NC=N3)[C@@H]5C[C@H]([C@H](C5)O)COS(=O)(=O)N.Cl

IIUPAC Name

[(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamate;hydrochloride

INCHI

1S/C21H25N5O4S.ClH/c22-31(28,29)30-11-14-9-15(10-19(14)27)26-8-7-17-20(23-12-24-21(17)26)25-18-6-5-13-3-1-2-4-16(13)18;/h1-4,7-8,12,14-15,18-19,27H,5-6,9-11H2,(H2,22,28,29)(H,23,24,25);1H/t14-,15+,18-,19-;/m0./s1

InChi Key

HJKDNNXKYODZJI-BVMPOVDASA-N

Smiles

C1CC2=CC=CC=C2C1NC3=C4C=CN(C4=NC=N3)C5CC(C(C5)O)COS(=O)(=O)N.Cl

PubChem CID

66576990

关联CAS

1160295-21-5

溶解性

DMSO : 100 mg/mL (208.34 mM; Need ultrasonic) H2O : 10 mg/mL (20.83 mM; Need ultrasonic)

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

479.139 Da

单同位素质量Monoisotopic Mass

479.139 Da

拓扑极表面积Topological Polar Surface Area

141.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

734

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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