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Plinabulin(NPI-2358)

Product Name
Plinabulin(NPI-2358)
CAS No.
714272-27-2
Chemical Name
Plinabulin(NPI-2358)
Synonyms
CS-829;NPI-2358;EOS-62083;NSC406141;Plinabulin;NSC 406141;NSC-406141;Plinabulin, >=98%;NPI-2358; NPI 2358;Plinabulin(NPI-2358)
CBNumber
CB92490824
Molecular Formula
C19H20N4O2
Formula Weight
336.39
MOL File
714272-27-2.mol
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Plinabulin(NPI-2358) Property

Density 
1.267
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

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

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N-Bromosuccinimide Price

Cayman Chemical
Product number
24190
Product name
Plinabulin
Purity
≥98%
Packaging
5mg
Price
$160
Updated
2024/03/01
Cayman Chemical
Product number
24190
Product name
Plinabulin
Purity
≥98%
Packaging
10mg
Price
$263
Updated
2024/03/01
Cayman Chemical
Product number
24190
Product name
Plinabulin
Purity
≥98%
Packaging
25mg
Price
$547
Updated
2024/03/01
Cayman Chemical
Product number
24190
Product name
Plinabulin
Purity
≥98%
Packaging
50mg
Price
$911
Updated
2024/03/01
ApexBio Technology
Product number
B2298
Product name
Plinabulin(NPI-2358)
Packaging
50mg
Price
$1126
Updated
2021/12/16
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Plinabulin(NPI-2358) Chemical Properties,Usage,Production

Definition

ChEBI: Plinabulin is a member of the class of 2,5-diketopiperazines that is piperazine-2,5-dione substituted by benzylidene and (5-tert-butyl-1H-imidazol-4-yl)methylidene groups at positions 3 and 6, respectively. It is a vascular disrupting agent and a microtubule destabalising agent which was in clinical trials (now discontinued) for the treatment of non-small cell lung cancer. It has a role as a microtubule-destabilising agent, an antineoplastic agent, an apoptosis inducer and an angiogenesis inhibitor. It is a member of 2,5-diketopiperazines, a member of imidazoles, a member of benzenes and an olefinic compound.

Biological Activity

the ic50 values of npi-2358 is 9.8 ± 2.4 nmol/l, 18 ± 5 nmol/l, 13 ± 1 nmol/l, 14 ± 2 nmol/l, 18 ± 1 nmol/l and 11 nmol/l for ht-29, du 145, pc-3, mda-mb-231, ncl-h292 and jurkat cell lines, respectively[1].plinabulin (npi-2358) is a vascular disrupting agent which binds to the colchicine-binding site of tubulin. npi-2358 could destabilize tumor vascular endothelial architectural resulting in selective collapse of established tumor vasculature [1].

in vitro

npi-2358 exhibited anti-tumor activity against various human tumor cell lines. in proliferating human umbilical vein endothelial cells (huvecs), administration of npi-2358 at 10 nmol/l induced tubulin depolymerization within 30 min [1]. in an in-vitro model of tumor vascular collapse, npi-2358 increased huvec monolayer permeability in a dose-dependent manner. plinabulin had also shown the in-vitro cytotoxic activity with ic50 values of 11 ± 5 nmol/l and 4.3 ± 2.2 nmol/l for mes-sa and hl-60 tumor cell lines, respectively[1].

in vivo

in the foot implanted c3h mammary carcinomas or leg implanted kht sarcomas mice model, 7.5 mg/kg plinabulin (intraperitoneally injected) significantly reduced the transfer constant (k(trans)) and the initial area under curve (iauc) within 1 hour after injection, reaching a lowest point at 3 h, but returning to normal within 24 h. a dose-dependent decrease in iauc and k(trans) was seen at 3 h. 12.5 mg/kg and 1.5 mg/kg npi-2358 showed significant anti-tumour effects in the c3h tumours and the kht sarcoma, respectively .

target

Tubulin

References

nicholson b1, lloyd gk, miller br, palladino ma, kiso y, hayashi y, neuteboom st. npi-2358 is a tubulin-depolymerizing agent: in-vitro evidence for activity as a tumor vascular-disrupting agent.anticancer drugs. 2006 jan; 17(1):25-31.bertelsen l b, shen y y, nielsen t, et al. vascular effects of plinabulin (npi-2358) and the influence on tumour response when given alone or combined with radiation[j]. international journal of radiation biology, 2011, 87(11): 1126-1134.millward m, mainwaring p, mita a, et al. phase 1 study of the novel vascular disrupting agent plinabulin (npi-2358) and docetaxel[j]. investigational new drugs, 2012, 30(3): 1065-1073.

Plinabulin(NPI-2358) Preparation Products And Raw materials

Raw materials

Preparation Products

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Plinabulin(NPI-2358) Suppliers

AdooQ BioScience, LLC
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+1 (866) 930-6790
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InvivoChem
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Aladdin Scientific
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ApexBio Technology
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View Lastest Price from Plinabulin(NPI-2358) manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Plinabulin 714272-27-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Plinabulin 714272-27-2
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-08
Career Henan Chemical Co
Product
Plinabulin(NPI-2358) 714272-27-2
Price
US $1.00/g
Min. Order
100drums
Purity
99%
Supply Ability
G/KG/T
Release date
2019-12-20

714272-27-2, Plinabulin(NPI-2358)Related Search:


  • Plinabulin(NPI-2358)
  • NPI-2358
  • Plinabulin
  • (3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione
  • NPI-2358 (Plinabulin)
  • (3Z,6Z)-3-benzylidene-6-((5-tert-butyl-1H-imidazol-4-yl)methylene)piperazine-2,5-dione
  • (3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione Plinabulin (NPI-2358)
  • Plinabulin (3Z,6Z)-3-[(5-tert-Butyl-1H-imidazol-4-yl)methylene]-6-(phenylmethylene)-2,5-piperazinedione
  • Plinabulin, >=98%
  • 3-(Z)-benzylidene-6-(((Z)-5-tert-butyl-1H-imidazol-4-yl)methylene)-piperazine-2,5-dione monohydrate
  • 2,5-Piperazinedione, 3-[[5-(1,1-dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-, (3Z,6Z)-
  • (Z)-3-((Z)-benzylidene)-6-((5-(tert-butyl)-1H-imidazol-4-yl)methylene)piperazine-2,5-dione
  • EOS-62083
  • NPI-2358; NPI 2358
  • CS-829
  • (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylidene]piperazine-2,5-dione
  • Plinabulin(NPI-2358)USP/EP/BP
  • NSC 406141
  • NSC406141
  • NSC-406141
  • Plinabulin NPI-2358 NPI2358
  • 714272-27-2
  • 714272-27-3
  • 714272-27-4
  • APIs
  • Inhibitors