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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Protein tyrosine kinase /JAK / STAT >JAK inhibitors >PACRITINIB

PACRITINIB

PACRITINIB Structure
  • ₹0
  • Product name: PACRITINIB
  • CAS: 937272-79-2
  • MF: C28H32N4O3
  • MW: 472.58
  • EINECS:
  • MDL Number:MFCD22572772
  • Synonyms:14,19-Dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 11-[2-(1-pyrrolidinyl)ethoxy]-, (16E)-;16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene Pacritinib (SB1518);Pacritinib, >=98%;PACRITINIB;SB1518;Pacritinib (SB1518);(16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene;SB1518(Pacritinib)
Manufacturer Product number Product description Packaging Price Updated Buy

Properties

Boiling point :694.3±65.0 °C(Predicted)
Density :1.22±0.1 g/cm3(Predicted)
storage temp. :Store at -20°C
solubility :DMSO:5.0(Max Conc. mg/mL);10.6(Max Conc. mM)
form :A crystalline solid
pka :9.56±0.20(Predicted)
color :Light yellow to yellow

Safety Information

Symbol(GHS): GHS hazard pictogramsGHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H373 May cause damage to organs through prolonged or repeated exposure Specific target organ toxicity, repeated exposure Category 2 Warning P260, P314, P501
H400 Very toxic to aquatic life Hazardous to the aquatic environment, acute hazard Category 1 Warning GHS hazard pictograms P273, P391, P501
H411 Toxic to aquatic life with long lasting effects Hazardous to the aquatic environment, long-term hazard Category 2
Precautionary statements:
P260 Do not breathe dust/fume/gas/mist/vapours/spray.
P273 Avoid release to the environment.
P314 Get medical advice/attention if you feel unwell.
P391 Collect spillage. Hazardous to the aquatic environment
P501 Dispose of contents/container to..…

Description

FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia. Pacritinib is an inhibitor of both FLT3 and JAK2 (IC50s = 22 and 23 nM, respectively). It also blocks the activities of the FLT3 D835Y mutant, FLT3 with internal tandem duplications (ITDs), and JAK2 with a V617F substitution (IC50s = 6, 20-180, and 220 nM, respectively). Pacritinib also inhibits JAK1, JAK3, and TYK2 (IC50s = 1280, 520, and 50 nM, respectively). Pacritinib is orally bioavailable, inhibiting FLT3 and JAK2 signaling, tumor growth, and metastasis in xenografts in mice. It is synergistic with the histone deacetylase inhibitor pracinostat (also known as SB 939, ), decreasing cell proliferation and inducing apoptosis in cells carrying either the JAK2 V617F mutation or FLT3 with ITDs, both in vitro and in vivo. Pacritinib has potential in resolving hematological malignancies.