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YLIU-5-162-1

Chemical Structure : YLIU-5-162-1

CAS No.: 2417685-83-5

YLIU-5-162-1

Catalog No.: PC-20901Not For Human Use, Lab Use Only.

YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

YLIU-4-105-1 is a novel type II JAK2 inhibitor, binds to JAK2 kinase domain (JH1), show potential for overcoming acquired resistance to ruxolitinib.
YLIU-4-105-1 shows pure JAK2 selectivity, inhibits pSTAT1 (Y701) and in some cases pERK1/2 (T202/Y204) to varying extents, but does not inhibit pAKT (T308).
YLIU-4-105-1 is more potent against JAK2 V617F-dependent SET2 cells.
YLIU-4-105-1 (50 mg/kg or 75 mg/kg, IP daily) shows abdominal ascites, intraabdominal drug precipitate, and dilated loops of bowel on rhEPO-induced polycythemia mouse model.

Physicochemical Properties

M.Wt 605.67
Formula C32H34F3N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(CC)CC2)=C1)C3=CC=C(C)C(C4=NN5C(C=C4)=NC(NC(C6CC6)=O)=C5)=C3

References

1. Matthew L Arwood, et al. Cell Chem Biol. 2023 Jun 15;30(6):618-631.e12.

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