Gandotinib (LY-2784544)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $980 | Check With Us |
| 500mg | $1350 | Check With Us |
| 1g | $2025 | Check With Us |
: Cat #: V0341 CAS #: 1229236-86-5 Purity ≥ 98%
Description: Gandotinib (formerly also known as LY2784544) is a novel, potent and selective JAK2 (Janus kinase) inhibitor with potential antitumor activity.
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| Molecular Weight (MW) | 469.94 |
|---|---|
| Molecular Formula | C23H25ClFN7O |
| CAS No. | 1229236-86-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 94 mg/mL (200.0 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 9 mg/mL (19.1 mM) | |
| SMILES Code | CC1=NNC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=CC=C(Cl)C=C5F)=C1 |
| Synonyms | LY-2784544; Gandotinib; LY 2784544; LY2784544; |
| Protocol | 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). |
|---|---|---|
| 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). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1279 mL | 10.6397 mL | 21.2793 mL | 42.5586 mL |
| 5mM | 0.4256 mL | 2.1279 mL | 4.2559 mL | 8.5117 mL |
| 10mM | 0.2128 mL | 1.0640 mL | 2.1279 mL | 4.2559 mL |
| 20mM | 0.1064 mL | 0.5320 mL | 1.0640 mL | 2.1279 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
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ddH2O,mix and clarify.
Note:
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