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Pacritinib

Pacritinib structure

CAS No:
937272-79-2
Formula:
C28H32N4O3
Chemical Name:
Pacritinib
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[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene;Pacritinib;SB 1518;1138325-13-9
Categories:
Biochemical Engineering > Inhibitors

Description

Pacritinib is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).

Pacritinib is under investigation for the prevention of Acute Myeloid Leukemia (AML).|Pacritinib is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Oral JAK2 inhibitor SB1518 competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity.

Pacritinib Basic Attributes

Molecular Weight：

472.59

Exact Mass：

472.58

UNII：

G22N65IL3O

NCI Thesaurus Code：

C78837

Characteristics

PSA：

68.7

XLogP3：

3.8

Density：

1.2±0.1 g/cm3

Boiling Point：

694.3±65.0°C at 760 mmHg

Flash Point：

384.0±35.7 °C

Refractive Index：

1.574

Drug Information

Drug Indication：

Treatment of post-essential thrombocythaemia myelofibrosis, Treatment of post-polycythaemia vera myelofibrosis

MeSH Entry Terms：

11-(2-pyrrolidin-1-ylethoxy)-14,19-dioxa-5,7,26-triazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene

Pacritinib Use and Manufacturing

Use Classification：

Human Drugs -> EU pediatric investigation plans

Computed Properties

Molecular Weight:472.6
XLogP3:3.8
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:4
Exact Mass:472.24744090
Monoisotopic Mass:472.24744090
Topological Polar Surface Area:68.7
Heavy Atom Count:35
Complexity:644
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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