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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-LY2784544
LY2784544

Chemical Structure : LY2784544

CAS No.: 1229236-86-5

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LY2784544 (LY 2784544;LY-2784544;Gandotinib)

货号: 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).

规格 价格 库存 数量
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 mg ￥3680 In stock
100 mg ￥5680 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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).

物理化学性质&存储条件

分子量 469.9423
分子式 C23H25ClFN7O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
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)-

参考文献

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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