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
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.
- InChIKey
- MPUQHZXIXSTTDU-QXGSTGNESA-N
- SMILES
- S(N)(OC[C@@H]1C[C@@H](N2C3C(C=C2)=C(N[C@@H]2C4=C(C=CC=C4)CC2)N=CN=3)C[C@@H]1O)(=O)=O
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.
N-Bromosuccinimide Price
- Product number
- 15217
- Product name
- MLN4924
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 15217
- Product name
- MLN4924
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $96
- Updated
- 2024/03/01
- Product number
- 15217
- Product name
- MLN4924
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $168
- Updated
- 2024/03/01
- Product number
- 6499
- Product name
- MLN4924
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $139
- Updated
- 2021/12/16
- Product number
- M425100
- Product name
- MLN4924
- Packaging
- 1mg
- Price
- $90
- Updated
- 2021/12/16
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
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View Lastest Price from Pevonedistat manufacturers
- 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
- 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
- Product
- Pevonedistat 905579-51-3
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 50000KG/month
- Release date
- 2024-10-10