Pevonedistat

Product Name: Pevonedistat
CAS No.: 905579-51-3
Chemical Name: Pevonedistat
Synonyms: MLN 4924;CS-821;TAK-924;Pevonedistat;mln4924 Free Base;PEVONEDISTAT;MLN-4924;MLN4924 (Pevonedistat);Pevonedistat (TAK-924);Pevonedistat (MLN-4924,TAK 924);Pevonedistat ISO 9001：2015 REACH
CBNumber: CB92510096
Molecular Formula: C21H25N5O4S
Formula Weight: 443.52
MOL File: 905579-51-3.mol

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Pevonedistat Property

Melting point:: 161-163°C
Boiling point:: 721.0±70.0 °C(Predicted)
Density: 1.62
storage temp.: -20°C Freezer
solubility: Soluble in DMSO (up to 10 mg/ml).
form: solid
pka: 9.35±0.70(Predicted)
color: White
Stability:: Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 15217
Product name: MLN4924
Purity: ≥98%
Packaging: 1mg
Price: $49
Updated: 2024/03/01

Cayman Chemical

Product number: 15217
Product name: MLN4924
Purity: ≥98%
Packaging: 5mg
Price: $96
Updated: 2024/03/01

Cayman Chemical

Product number: 15217
Product name: MLN4924
Purity: ≥98%
Packaging: 10mg
Price: $168
Updated: 2024/03/01

Tocris

Product number: 6499
Product name: MLN4924
Purity: ≥98%(HPLC)
Packaging: 10
Price: $139
Updated: 2021/12/16

TRC

Product number: M425100
Product name: MLN4924
Packaging: 1mg
Price: $90
Updated: 2021/12/16

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Pevonedistat Chemical Properties,Usage,Production

Description

MLN4924 (905579-51-3) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor.1?It disrupts cullin-RING ligase-mediated protein turnover leading to apoptosis in human tumor cells. Suppresses the growth of human tumor xenografts in mice.2?Upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma.3?Modulates tumor microenvironment.4?Cell permeable.

Chemical Properties

White Solid

Uses

A potent and selective inhibitor of NAE. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. The ubiquitin-proteasome pathway mediates the destruction of unwanted proteins. Potent NAE inhibitor; NEDD8 E1 Activating Enzyme Inhibitor.

Definition

ChEBI: Pevonedistat is a pyrrolopyrimidine that is 7H-pyrrolo[2,3-d]pyrimidine which is substituted by a (1S)-2,3-dihydro-1H-inden-1-ylnitrilo group at position 4 and by a (1S,3S,4S)-3-hydroxy-4-[(sulfamoyloxy)methyl]cyclopentyl group at position 7. It is a potent and selective NEDD8-activating enzyme inhibitor with an IC50 of 4.7 nM, and currently under clinical investigation for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndromes. It has a role as an apoptosis inducer and an antineoplastic agent. It is a pyrrolopyrimidine, a secondary amino compound, a member of cyclopentanols, a sulfamidate and a member of indanes.

Enzyme inhibitor

This first-in-class small molecule inhibitor (FW = 443.52 g/mol; CAS 905579-51-3; Solubility = 10 mg/mL DMSO), also named MLN4924 and [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3- d]pyrimidin-7-yl]-2-hydroxycyclopentyl]sulfamate methyl ester, targets Nedd8 activating enzyme, or NAE (IC50 = 4.7 nM), with much weaker action against UAE (IC50 = 1.5 μM), SAE (IC50 = 8.2 μM), and UBA6 (IC50 = 1.8 μM). In most cancer cells, pevonedistat treatment results in the induction of DNA re-replication, resulting in DNA damage and cell death. MLN4924 also exhibits an alternative mechanism of action. Treatment of activated B cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cells with pevonedistat resulted in rapid accumulation of pIkBa, decrease in nuclear p65 content, reduction of transcriptional activity of NF-kB (or nuclear factor k-light-chain-enhancer of activated B cells), and G1 arrest, ultimately resulting in apoptosis induction, events consistent with potent NF-kB pathway inhibition. Treatment of germinal-center B cell-like (GCB) DLBCL cells resulted in an increase in cellular Cdt-1 and accumulation of cells in S-phase, consistent with cells undergoing DNA rereplication. Pevonedistat also inhibits Vpx/Vpr-induced SAMHD1 degradation by inhibiting the neddylation of E3 ubiquitin-ligase and blocking SIVmac replication in myeloid cells, therebyindicating the potential efficacy of inhibiting neddylation as an antiretroviral strategy

storage

Store at -20°C

References

1) Soucy, et al. (2009), An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature 458 732 2) Milhollen, et al. (2010) MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF-(kappa)B-dependent lymphoma. Blood, 116 1515 3) Zhou et al. (2019) Neddylation inhibition upregulates PD-L1 expression and enhances the efficacy of immune checkpoint blockade in glioblastoma; Int. J. Cancer, 145 763 4) Zhou et al. (2019) Neddylation: a novel modulator of the tumor microenvironment; Mol. Cancer 18 77

Pevonedistat Preparation Products And Raw materials

Raw materials

Preparation Products

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Pevonedistat Suppliers

Canada 2 China 126 India 1 United States 20 Global 149

MedChemexpress LLC

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View Lastest Price from Pevonedistat manufacturers

Wuhan Haorong Biotechnology Co.,Ltd

Product: Pevonedistat 905579-51-3
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 5000
Release date: 2023-08-07

Career Henan Chemica Co

Product: Pevonedistat 905579-51-3
Price: US $1.00/g
Min. Order: 1g
Purity: 85.0-99.8%
Supply Ability: 20tons
Release date: 2020-10-29

Hebei Mojin Biotechnology Co., Ltd

Product: Pevonedistat 905579-51-3
Price: US $0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 50000KG/month
Release date: 2024-10-10

905579-51-3, PevonedistatRelated Search:

MLN9708 MLN-4760 MLN-8237 TYRPHOSTIN AG 1296 Imatinib mesylate Troglitazone Cantharidin N,N-DIETHYLBENZAMIDE

((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)aMino)-7H-pyrrolo[2,3-d]pyriMidin-7-yl)-2-hydroxycyclopentyl)Methyl sulfaMate

[(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 sulfaMate

CS-821

TAK-924

PEVONEDISTAT;MLN-4924

Pevonedistat

MLN4924 (Pevonedistat)

Sulfamic acid [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimi

MLN 4924

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

mln4924 Free Base

Pevonedistat (MLN-4924,TAK 924)

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

(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

Pevonedistat (TAK-924)

Pevonedistat ISO 9001：2015 REACH

905579-51-3

C21H25N5O4S

Bases & Related Reagents

Carbohydrates & Derivatives

Heterocycles

Inhibitors

Intermediates & Fine Chemicals

Nucleotides

Pharmaceuticals