WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406429
CAS#: 423148-78-1
Description: PYZD-4409 is an inhibitor of ubiquitin-activating enzyme UBA1 (E1). 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. Mechanistically, genetic or chemical inhibition of E1 increased expression of E1 stress markers. Moreover, BI-1 overexpression blocked cell death after E1 inhibition, suggesting ER stress is functionally important for cell death after E1 inhibition. Finally, in a mouse model of leukemia, intraperitoneal administration of PYZD - 4409 decreased tumor weight and volume compared with control without untoward toxicity.
MedKoo Cat#: 406429
Name: PYZD-4409
CAS#: 423148-78-1
Chemical Formula: C14H7ClFN3O5
Exact Mass: 351.00583
Molecular Weight: 351.67
Elemental Analysis: C, 47.81; H, 2.01; Cl, 10.08; F, 5.40; N, 11.95; O, 22.75
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
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 |
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. PubMed PMID: 20075161; PubMed Central PMCID: PMC2920204.
