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
- Molecular Weight:
- 443.52
- MOL File:
- 905579-51-3.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/8/7 22:27:18
| 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. |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319 | |||||||||
| Precautionary statements | P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313 | |||||||||
| NFPA 704 |
|
Pevonedistat Chemical Properties,Uses,Production
Chemical Properties
White Solid
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
Pevonedistat Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Wuhan Haorong Biotechnology Co.,ltd | +86-18565342920; +8618565342920 | China | 289 | 58 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49392 | 58 | Inquiry |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 | China | 30250 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 24200 | 58 | Inquiry |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | China | 9640 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
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