Structure
LY2784544, Inhibitor
LY2784544
Purity
>98% (HPLC)
Synonyms
LY2784544; LY 2784544; LY-2784544; Gandotinib; inhibitor
Purity/Purification
>98% (HPLC)
Suitability
10mM in DMSO
Target
JAK
Receptor
FLT3; JAK1; JAK2; JAK2 (V617F)
Chemical Name
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)
SMILES
CC1=NNC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=CC=C(Cl)C=C5F)=C1
Molecular Formula
C23H25ClFN7O
CAS Number
1229236-86-5
Preparation and Storage
Store at -20 degree C
Stability: >=2 years
Shipping: Ice Pack
Stability: >=2 years
Shipping: Ice Pack
Structure
Structure
Related Product Information for LY2784544, inhibitor
LY2784544 (Gandotinib) is a potent, selective and ATP-competitive inhibitor of JAK2V617F, effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55nM, respectively); inhibits JAK2 and JAK3 in biochemical assays with IC50 of 3nM and 48nM, respectively; LY2784544 is much less potent at inhibiting IL-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309nM, respectively); effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells (TED50=12.7mg/kg) and significantly reduces Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model; also is a potent GPR39 agonist with pEC50 of 9.36 (at 316uM ZnCl2). Blood Cancer Phase 2 Clinical
Product Categories/Family for LY2784544, inhibitor
References
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.
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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Product Notes
The LY2784544 (Catalog #AAA3600896) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "LY2784544, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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