Home Cart Sign in  
Chemical Structure| 714272-27-2 Chemical Structure| 714272-27-2

Structure of Plinabulin
CAS No.: 714272-27-2

Chemical Structure| 714272-27-2

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Plinabulin is a vascular disrupting agent (VDA) against tubulin-depolymerizing with IC50 of 9.8~18 nM in tumor cells.

Synonyms: NPI-2358

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Plinabulin

CAS No. :714272-27-2
Formula : C19H20N4O2
M.W : 336.39
SMILES Code : O=C(/C(NC/1=O)=C/C2=CC=CC=C2)NC1=C/C3=C(C(C)(C)C)NC=N3
Synonyms :
NPI-2358
MDL No. :MFCD18074510

Safety of Plinabulin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Plinabulin

cytoskeleton

Isoform Comparison

Biological Activity

Description
Plinabulin (NPI-2358) acts as a vascular disrupting agent and inhibits tubulin depolymerization with an IC50 of 9.8 nM in HT-29 cells[1].
Target
  • VDA

    Tubulin, IC50:9.8 nM-18 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
XS106 cells 200 nM 20 hours To evaluate the effect of Plinabulin on the maturation of XS106 cells, results showed that Plinabulin significantly induced the expression of CD80 and CD86 Cell Rep. 2019 Sep 24;28(13):3367-3380.e8.
Splenic DCs 100 nM 20 hours To evaluate the effect of Plinabulin on the maturation of splenic DCs, results showed that Plinabulin significantly induced the expression of CD80 and CD86 Cell Rep. 2019 Sep 24;28(13):3367-3380.e8.
SP37A3 cells 100 nM 20 hours To evaluate the effect of Plinabulin on the maturation of SP37A3 cells, results showed that Plinabulin significantly induced the expression of CD80 and CD86 Cell Rep. 2019 Sep 24;28(13):3367-3380.e8.
HT-29 human colon cancer cells 2 nM (Z-1), 20 nM (Z-2), 200 nM (Z-3) 6 hours Assessed microtubule network disruption via immunofluorescence imaging, showing Z-isomers induced abnormal tubulin aggregation at respective concentrations. Nat Commun. 2022;13(1):6066.
Healthy human monocyte-derived macrophages 200 nM and 1000 nM 48 or 72 hours To evaluate the effect of Plinabulin on human macrophage polarization. Results showed that Plinabulin treatment resulted in a dose-dependent increase in expression of CD80, a decrease of the M2 marker expression and a significant increase in the M1/M2 ratio. Front Oncol. 2021 Mar 3;11:644608.
Murine bone marrow-derived macrophages (BMDM) 200 nM and 1000 nM 48 or 72 hours To evaluate the effect of Plinabulin on macrophage polarization. Results showed that Plinabulin treatment led to a significant, dose-dependent increase in M1 markers CD80 and CD86 and a concomitant decrease in expression of CD206. Front Oncol. 2021 Mar 3;11:644608.
HepaRG Cells Cryopreserved 30 μM 2 hours Evaluation of Plinabulin metabolites in HepaRG cells, identifying 2 phase-II sulfate conjugate metabolites. ACS Omega. 2022 Jun 14;7(25):21465-21472.
Human liver microsomes (HLMs) 30 μM 90 minutes Evaluation of Plinabulin metabolites in the presence of NADPH, identifying 17 phase-I metabolites including isomerization, hydroxylation, hydration, and oxygenation products. ACS Omega. 2022 Jun 14;7(25):21465-21472.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6N wild-type mice and C57BL/6N Rag2−/− mice Subcutaneous MC38 colon cancer model Peritumoral injection 7.0 mg/kg Seven doses over 11 days To evaluate the effect of Plinabulin on tumor growth and macrophage polarization in the tumor microenvironment. Results showed that Plinabulin treatment significantly inhibited tumor growth and increased the proportion of M1-like TAMs in the tumor. Front Oncol. 2021 Mar 3;11:644608.
Wistar rats Leukopenia model Intravenous injection 0.5 mg/kg, 1 mg/kg, 3 mg/kg Single dose, observed for 10 hours To investigate the pharmacokinetic differences of Plinabulin between leukopenic and normal rats. Results showed no significant pharmacokinetic differences between the leukopenic and normal groups. Pharmaceuticals (Basel). 2023 Aug 14;16(8):1153
Zebrafish larvae Zebrafish PTZ seizure model Water immersion 1.25–10 µM 2 hours or 18 hours Evaluate the antiseizure activity of Plinabulin, showing significant reduction in PTZ-induced seizure behavior after 18 hours of treatment Pharmaceuticals (Basel). 2022 Feb 18;15(2):247

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05130827 Multiple Myeloma PHASE2 ACTIVE_NOT_RECRUITING 2025-11-25 Memorial Sloan Kettering Baski... More >>ng Ridge (Limited Protocol Activities), Basking Ridge, New Jersey, 07920, United States|Memorial Sloan Kettering Monmouth (Limited Protocol Activities), Middletown, New Jersey, 07748, United States|Memorial Sloan Kettering Bergen (Limited Protocol Activities), Montvale, New Jersey, 07645, United States|Memorial Sloan Kettering Cancer Center @ Suffolk-Commack (Limited protocol activities), Commack, New York, 11725, United States|Memorial Sloan Kettering Westchester (Limited Protocol Activities), Harrison, New York, 10604, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Memorial Sloan Kettering Nassau (Limited protocol activities), Rockville Centre, New York, 11553, United States Less <<
NCT00322608 Cancer PHASE1 COMPLETED 2025-12-09 Barbara Ann Karmanos Cancer In... More >>stitute/Wayne State University, Detroit, Michigan, 48201, United States|Institute for Drug Development, San Antonio, Texas, 78245-3217, United States|Northwest Medical Specialties, Tacoma, Washington, 98405, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.97mL

0.59mL

0.30mL

14.86mL

2.97mL

1.49mL

29.73mL

5.95mL

2.97mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

Categories