| Identification | Back Directory | [Name]
Benzenesulfonamide, 2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)-1H-pyrazol-4-yl]-4-[2-(1-piperazinyl)-4-pyridinyl]- | [CAS]
1215011-08-7 | [Synonyms]
PCLX-001
Benzenesulfonamide, 2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)-1H-pyrazol-4-yl]-4-[2-(1-piperazinyl)-4-pyridinyl]- | [Molecular Formula]
C24H30Cl2N6O2S | [MOL File]
1215011-08-7.mol | [Molecular Weight]
537.51 |
| Chemical Properties | Back Directory | [Boiling point ]
704.4±70.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
6.97±0.50(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Zelenirstat is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. Zelenirstat can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma[1][2]. | [in vivo]
Zelenirstat (5-1000 mg/kg, oral, once daily, 14-21 days) has an MTD of 50 mg/kg in a 21-day study in mice, >75 mg/kg in a 14-day study in rats, and between 5 and 25 mg/kg in a 14-day study in dogs[1].
Zelenirstat (0-50 mg/kg, subcutaneous injection, once daily; 0-15 days) induces tumor regression in BL2 xenograft mice[2]. | Animal Model: | Mice, rats, dogs[1] | | Dosage: | 5-1000 mg/kg; daily; 14 and 21 days | | Administration: | Oral | | Result: | Showed that a single dose of 50 mg/kg caused vomiting, diarrhea, and weight loss in dogs, while a single dose of 1000 mg/kg caused the death of one rat and complete regression of xenograft tumors in mice. |
| Animal Model: | BL2 xenograft mice[2] | | Dosage: | 0, 10, 20, 50 mg/kg; daily; 0, 5, 10, 15 days | | Administration: | Subcutaneous injection (s.c.) | | Result: | Reduced tumor volume and caused complete tumor regression, and prolonged the survival of BL2 tumor-bearing mice. |
| [storage]
Store at -20°C | [References]
[1] Michael Weickert, et al. Initial Characterization and Toxicology of an Nmt Inhibitor in Development for Hematologic Malignancies. Blood. 2019. 134(s1):3362.
[2] Beauchamp E, et al. Targeting N-myristoylation for therapy of B-cell lymphomas. Nat Commun. 2020 Oct 22;11(1):5348. DOI:10.1038/s41467-020-18998-1 |
|
| Company Name: |
nanjing
|
| Tel: |
13376082704 13376082704 |
| Website: |
www.linye-e.com/ |
|