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
- Molecular Weight:
- 336.39
- MDL Number:
- MFCD18074510
- MOL File:
- 714272-27-2.mol
- MSDS File:
- SDS
| Density | 1.267 |
|---|---|
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| form | Powder |
| color | Light yellow to yellow |
| FDA UNII | 986FY7F8XR |
| NCI Drug Dictionary | plinabulin |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Plinabulin(NPI-2358) price More Price(14)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 24190 | Plinabulin ≥98% | 714272-27-2 | 5mg | $160 | 2024-03-01 | Buy |
| Cayman Chemical | 24190 | Plinabulin ≥98% | 714272-27-2 | 10mg | $263 | 2024-03-01 | Buy |
| Cayman Chemical | 24190 | Plinabulin ≥98% | 714272-27-2 | 25mg | $547 | 2024-03-01 | Buy |
| Cayman Chemical | 24190 | Plinabulin ≥98% | 714272-27-2 | 50mg | $911 | 2024-03-01 | Buy |
| ApexBio Technology | B2298 | Plinabulin(NPI-2358) | 714272-27-2 | 50mg | $1126 | 2021-12-16 | Buy |
Plinabulin(NPI-2358) Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32965 | 60 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49732 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29809 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 22787 | 58 |
| Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 | gksales1@gk-bio.com | China | 9310 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| Henan Alfa Chemical Co., Ltd | China | 13196 | 58 | ||
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
View Lastest Price from Plinabulin(NPI-2358) manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2021-07-13 | Plinabulin
714272-27-2
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd | |
 |
2021-07-09 | Plinabulin
714272-27-2
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd | |
 |
2019-12-23 | Plinabulin(NPI-2358)
714272-27-2
|
US $1.00 / g | 100drums | 99% | G/KG/T | Career Henan Chemical Co |
-
- Plinabulin
714272-27-2
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
-
- Plinabulin
714272-27-2
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
-
- Plinabulin(NPI-2358)
714272-27-2
- US $1.00 / g
- 99%
- Career Henan Chemical Co