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LY2784544 | JAK2 inhibitor

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Price:
$169.00
Catalog #:
C5178-5
Quantity:


Product Description

LY-2784544 is an orally-available, imidazolopyridazine-based inhibitor of the JAK2-V617F mutation, the most common abnormality in Bcr-Abl-negative myeloid proliferative neoplasms. [1] Inhibition in Ba/F3 cells was found to be 55 nM. [2] Inhibition of wild-type JAK2 was minimal (IC50 = 2.3 uM), such that normal marrow function is not impeded. [2, 3]

Antiproliferation activity of LY-2784544 in JAK2-V617F-driven cells was shown to be 68 nM. [2]. In Ba/F3 xenografts, LY-2784544 inhibits STAT5 phosphorylation at an threshhold effective dose (TED50) of 12.7 mg/kg. [2]


Technical information:

Chemical Formula:   C23H25ClFN7O
CAS #:   1229236-86-5
Molecular Weight:   469.94
Purity:   > 98%
Appearance:   White
Chemical Name:   3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine
Solubility:   Up to 100 mM in DMSO
Synonyms:   LY-2784544, LY 2784544, LY2784544

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Mitchell et al., Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544. Org. Process Res. Dev. 2012, 15, 70-81.
2. Ma et al., 4087 Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models. 53rd ASH Annual Meeting and Exposition, 2011, Abstract 4087.
3. "Lilly oncology reveals findings from study of JAK2 inhibitor for blood cancers at ASH meeting" Eli Lilly ASH review, Dec. 11, 2012.

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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