Antibodies
LY2784544
- 貨號 Cat. No.
- S2179
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
LY2784544
LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. | |||||
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| Targets | JAK2 | JAK2 | JAK2V617F | |||
| IC50 | 3 nM | 0.288 nM (Ki) | 0.245 nM (Ki) [1] | |||
| In vitro | LY2784544 also inhibits IL-3-activated wild type JAK2 with IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows antiproliferation activity in JAK2 V617F-driven cells with IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. [1] Though biochemical assays do not reveal selectivity of LY2784544 for mutant JAK2V617F, LY2784544 shows higher selectivity for inhibition of JAK2-mediated signaling and induction of apoptosis in Ba/F3 cells expressing JAK2V617F than wild-type cells. [2] | |||||
| In vivo | LY2784544 significantly inhibits STAT5 phosphorylation in Ba/F3-JAK2 V617F-GFP xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces Ba/F3-JAK2 V617F-GFP tumor burden in the JAK2 V617F-induced MPN model with a TED50 of 13.7 mg/kg after oral treatment. LY2784544 has no effect on CD71/Ter119 positive erythroid progenitors in spleens of SCID mice after oral treatment. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01134120 | Active, not recruiting | Myeloproliferative Disorders|Thrombocythemia, Essential|Polycythemia Vera|Primary Myelofibrosis | Eli Lilly and Company | 2010-04 | Phase 1 |
| NCT01577355 | Completed | Healthy Male Volunteers | Eli Lilly and Company | 2012-04 | Phase 1 |
| NCT01594723 | Recruiting | Neoplasms, Hematologic | Eli Lilly and Company | 2012-05 | Phase 2 |
| NCT01520220 | Recruiting | Myeloproliferative Neoplasms of|Polycythemia Vera|Essential Thrombocythemia|Myelofibrosis | Eli Lilly and Company | 2012-06 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 469.94 |
|---|---|
| Formula | C23H25ClFN7O |
| CAS No. | 1229236-86-5 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 94 mg/mL (200 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 9 mg/mL (19 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 3-(4-chloro-2-fluorobenzyl)-2-methyl-N-(3-methyl-1H-pyrazol-5-yl)-8-(morpholinomethyl)imidazo[1,2-b]pyridazin-6-amine |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.46994 | 4.6994 | 9.3988 | 14.0982 |
Customer Reviews (1)
 Click to enlarge | Rating | |
| Source | M.Sc. Karoline Gaebler and Dr. Claude Haan of Université du Luxembourg. LY2784544 purchased from Selleck | |
| Method | Western blot | |
| Cell Lines | HEL cells | |
| Concentrations | ||
| Incubation Time | 3 h | |
| Results | LY2784544 inhibits Jak2-V617F mediated signal transduction at submicromolar concentrations in intact cells. |
