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Chemical Structure : LY2784544
CAS No.: 1229236-86-5
Catalog No.: PC-43343Not For Human Use, Lab Use Only.
LY2784544 (Gandotinib) is a potent, selective and ATP-competitive inhibitor of JAK2 V617F, effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $368 | In stock | |
| 100 mg | $568 | In stock | |
| 250 mg | Get quote |
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LY2784544 (Gandotinib) is a potent, selective and ATP-competitive inhibitor of JAK2 V617F, effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively).
LY2784544 inhibits JAK2 and JAK3 in biochemical assays with IC50 of 3 nM and 48 nM, respectively.
LY2784544 is much less potent at inhibiting IL-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309 nM, respectively).
LY2784544 effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduces Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model.
LY2784544 also is a potent GPR39 agonist with pEC50 of 9.36 (at 316 uM ZnCl2).
| M.Wt | 469.9423 | |
| Formula | C23H25ClFN7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Imidazo[1,2-b]pyridazin-6-amine, 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)- |
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1. Ma L, et al. Blood Cancer J. 2013 Apr 12;3:e109.
2. Telford BJ, et al. Mol Cancer Ther. 2015 May;14(5):1213-23.
3. Gunerka P, et al. Eur J Pharmacol. 2015 Oct 15;765:188-97.
4. Sato S, et al. Mol Pharmacol. 2016 Dec;90(6):726-737.
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