Synonym
PYZD4409; PYZD 4409; PYZD-4409;
IUPAC/Chemical Name
1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furyl)methylene]-3,5-pyrazolidinedione
InChi Key
MSYMKEYWUWVZQY-TWGQIWQCSA-N
InChi Code
InChI=1S/C14H7ClFN3O5/c15-10-5-7(1-3-11(10)16)18-14(21)9(13(20)17-18)6-8-2-4-12(24-8)19(22)23/h1-6H,(H,17,20)/b9-6-
SMILES Code
O=C(/C1=C/C2=CC=C([N+]([O-])=O)O2)NN(C3=CC=C(F)C(Cl)=C3)C1=O
Appearance
white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
PYZD-4409 blocks the degradation of p53 and cyclin D3. PYZD-4409 inhibits NF-κB activation and induces cell death associated with ER stress.
In vitro activity:
To be determined
In vivo activity:
In a mouse model of leukemia, intraperitoneal administration of PYZD-4409 decreased tumor weight and volume compared with control without untoward toxicity. PYZD-4409 induced cell death in malignant cells and preferentially inhibited the clonogenic growth of primary acute myeloid leukemia cells compared with normal hematopoietic cells.
Reference: Blood. 2010 Mar 18;115(11):2251-9. https://pubmed.ncbi.nlm.nih.gov/20075161/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
10.0 |
28.44 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
351.67
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Xu GW, Ali M, Wood TE, Wong D, Maclean N, Wang X, Gronda M, Skrtic M, Li X, Hurren R, Mao X, Venkatesan M, Beheshti Zavareh R, Ketela T, Reed JC, Rose D, Moffat J, Batey RA, Dhe-Paganon S, Schimmer AD. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010 Mar 18;115(11):2251-9. doi: 10.1182/blood-2009-07-231191. Epub 2010 Jan 14. PMID: 20075161; PMCID: PMC2920204.
In vitro protocol:
To be determined
In vivo protocol:
1. Xu GW, Ali M, Wood TE, Wong D, Maclean N, Wang X, Gronda M, Skrtic M, Li X, Hurren R, Mao X, Venkatesan M, Beheshti Zavareh R, Ketela T, Reed JC, Rose D, Moffat J, Batey RA, Dhe-Paganon S, Schimmer AD. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010 Mar 18;115(11):2251-9. doi: 10.1182/blood-2009-07-231191. Epub 2010 Jan 14. PMID: 20075161; PMCID: PMC2920204.
Xu GW, Ali M, Wood TE, Wong D, Maclean N, Wang X, Gronda M, Skrtic M, Li X, Hurren R, Mao X, Venkatesan M, Beheshti Zavareh R, Ketela T, Reed JC, Rose D, Moffat J, Batey RA, Dhe-Paganon S, Schimmer AD. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood. 2010 Mar 18;115(11):2251-9. doi: 10.1182/blood-2009-07-231191. Epub 2010 Jan 14. PMID: 20075161; PMCID: PMC2920204.
Xu, W., Lukkarila, J. L., da Silva, S. R., Paiva, S. L., Gunning, P. T., & Schimmer, A. D. (2013). Targeting the ubiquitin E1 as a novel anti-cancer strategy. Current pharmaceutical design, 19(18), 3201-3209.
Kleynhans, A. (2021). Therapeutically targeting USP5 in MYCN-driven neuroblastoma (Doctoral dissertation, UNSW Sydney).
