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Pacritinib

Cat. No. M2912
Pacritinib  Structure
Synonym:

SB1518

Size Price Availability Quantity
2mg USD 90  USD90 In stock
5mg USD 140  USD140 In stock
10mg USD 258  USD258 In stock
50mg USD 1120  USD1120 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Pacritinib (SB1518) is an effective mutant inhibitor of wild-type JAK2 and JAK2V617F with IC50 of 23 nM and 19 nM, respectively. Pacritinib also inhibited FLT3 and its mutant FLT3D835Y with IC50 of 22 nM and 6 nM, respectively.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 472.58
Formula C28H32N4O3
CAS Number 937272-79-2
Purity >98%
Solubility DMSO
Storage at -20°C
References

[1] Annkristin Heine, et al. Pacritinib protects dendritic cells more efficiently than ruxolitinib

[2] Douglas Tremblay, et al. Pacritinib to treat myelofibrosis patients with thrombocytopenia

[3] John Mascarenhas, et al. Pacritinib vs Best Available Therapy, Including Ruxolitinib, in Patients With Myelofibrosis: A Randomized Clinical Trial

[4] Ruben A Mesa, et al. Pacritinib versus best available therapy for the treatment of myelofibrosis irrespective of baseline cytopenias (PERSIST-1): an international, randomised, phase 3 trial

[5] Yan Beauverd, et al. Pacritinib: a new agent for the management of myelofibrosis?

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  Catalog
Abmole Inhibitor Catalog




Keywords: Pacritinib , SB1518 supplier, JAK, inhibitors

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