LY2784544
Modify Date: 2024-01-04 12:37:52
LY2784544 structure
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Common Name | LY2784544 | ||
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| CAS Number | 1229236-86-5 | Molecular Weight | 469.942 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C23H25ClFN7O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of LY2784544Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM. |
| Name | 3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine |
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| Synonym | More Synonyms |
| Description | Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM. |
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| Related Catalog | |
| Target |
JAK2:3 nM (IC50) FGFR2:32 nM (IC50) Flt-4:25 nM (IC50) Tyk2:44 nM (IC50) JAK3:48 nM (IC50) FGFR3:106 nM (IC50) KDR:109 nM (IC50) FLT3:4 nM (IC50) TRKB:95 nM (IC50) ALK:138 nM (IC50) MUSK:147 nM (IC50) AURKA:168 nM (IC50) MAP3K9:299 nM (IC50) |
| In Vitro | Gandotinib (LY2784544), a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase. LY2784544 effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively). In comparison, Gandotinib (LY2784544) is much less potent at inhibiting interleukin-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309 nM, respectively). Gandotinib (LY2784544) potently inhibits the JAK2V617F signaling (IC50=20 nM) but, remarkably, shows very minimal activity against the IL-3-activated wild-type JAK2 signaling with an IC50 of 1183 nM. LY2784544 inhibits the proliferation of JAK2V617F-expressing cells (IC50=55 nM) and is markedly less potent as an inhibitor of the proliferation of IL-3-stimulated wild-type JAK2 expressing Ba/F3 cells (IC50=1309 nM). Gandotinib (LY2784544) is potent in the cell-based TF-1 JAK2 assay (IC50=45 nM) and had the desired threshold selectivity in the NK-92 JAK3/JAK1 heterodimer assay (942 nM)[1]. |
| In Vivo | Gandotinib (LY2784544) effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP (green fluorescent protein) ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduces (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED50=13.7 mg/kg, twice daily)[1]. |
| Cell Assay | Ba/F3 cells expressing JAK2V617F are placed in RPMI-1640-containing vehicle (DMSO) or Gandotinib (LY2784544) (concentration range, 0.001-20 μM) (1×104 cells/96-well). Ba/F3 cells expressing wild-type JAK2 are treated similarly except IL-3 (2 ng/mL) is added. After a 72-hour incubation, cell proliferation is assessed by adding Cell Titer 96 Aqueous One Solution Reagent (20 μL/well). The IC50 for inhibition of cell proliferation is calculated using the GraphPad Prism 4 software[1]. |
| Animal Admin | Mice[1] Dose- and time-dependent in vivo inhibition of JAK2V617F signaling is assessed by measuring inhibition of STAT5 phosphorylation in a mouse ascitic tumor model. Ba/F3-JAK2V617F-GFP cells (1×107) are implanted in the intraperitoneal cavity of severe combined immunodeficiency mice (SCID mice) and allowed to develop into ascitic tumors for 7 days. For dose-response studies (six animals/group), Gandotinib (LY2784544) is administered once by oral gavage (2.5, 5, 10, 20, 40, or 80 mg/kg), then 30 min later, ascitic tumor cells are collected, fixed, incubated for 2 h with Mouse-anti-pSTAT5 (pY694) Alexa Fluor 647 (1:10 dilution), and analyzed by flow cytometry. Time course studies are performed similarly, except the animals are treated with Gandotinib (LY2784544) at 20, 40 or 80 mg/kg and ascitic tumor cells collected at prespecified intervals of 0.25-6 h after dosing. Data are analyzed by the one-way analysis of variance, and Dunnett's test (α=0.05). Dose response data are analyzed with a four-parameter logistic curve-fitting program. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C23H25ClFN7O |
| Molecular Weight | 469.942 |
| Exact Mass | 469.179321 |
| PSA | 86.60000 |
| LogP | 2.39 |
| Index of Refraction | 1.700 |
| Storage condition | -20°C |
| Hazard Codes | Xi |
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~97%
LY2784544 CAS#:1229236-86-5 |
| Literature: Mitchell, David; Cole, Kevin P.; Pollock, Patrick M.; Coppert, David M.; Burkholder, Timothy P.; Clayton, Joshua R. Organic Process Research and Development, 2012 , vol. 16, # 1 p. 70 - 81 |
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LY2784544 CAS#:1229236-86-5 |
| Literature: Organic Process Research and Development, , vol. 16, # 1 p. 70 - 81 |
|
~%
LY2784544 CAS#:1229236-86-5 |
| Literature: Organic Process Research and Development, , vol. 16, # 1 p. 70 - 81 |
|
~%
LY2784544 CAS#:1229236-86-5 |
| Literature: Organic Process Research and Development, , vol. 16, # 1 p. 70 - 81 |
|
~%
LY2784544 CAS#:1229236-86-5 |
| Literature: Organic Process Research and Development, , vol. 16, # 1 p. 70 - 81 |
|
~%
LY2784544 CAS#:1229236-86-5 |
| Literature: Organic Process Research and Development, , vol. 16, # 1 p. 70 - 81 |
![6-chloro-3-(4-chloro-2-fluorobenzyl)-2-Methyl-8-(Morpholin-4-ylmethyl)imidazo[1,2-b]pyridazine structure](https://www.chemsrc.com/caspic/336/1229236-85-4.png)
![(4-CHLORO-2-FLUOROPHENYL)(6-CHLORO-2-METHYL-8-(MORPHOLINOMETHYL)IMIDAZO[1,2-B]PYRIDAZIN-3-YL)METHANONE structure](https://www.chemsrc.com/caspic/412/1229236-83-2.png)
![(4-chloro-2-fluorophenyl)(6-chloro-2-methylimidazo-[1,2-b]pyridazin-3-yl)methanone structure](https://www.chemsrc.com/caspic/036/1229236-80-9.png)
| cc-18 |
| Gandotinib [USAN] |
| 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)- |
| 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine |
| Gandotinib |
| S2179_Selleck |
| 3-(4-Chloro-2-fluorobenzyl)-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)imidazo[1,2-b]pyridazin-6-amine |
| LY2784544 |
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: LY2784544
- Price: ￥1248.0/5mg ￥1748.0/10mg
- Purity: 98.0%
- Stocking Period: 2 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Gandotinib(LY2784544)
- Price: $450.0/100mg $900.0/250mg $1800.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- Dayang Chem (Hangzhou) Co., Ltd.
- China
- Product Name: INK-128
- Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Ms Wang
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Price: $145/10mM*1mLinDMSO
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