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LY2784544, JAK2 inhibitor

LY2784544, JAK2 inhibitor

$129.00
A highly potent and selective mutant JAK2 (V617F) inhibitor.
Catalog No. Unit Price Qty
M60079-5s 5mg solid $129.00
M60079-25s 25mg solid $650.00

Details

Product Information
Molecular Weight: 469.94
Formula: C23H25ClFN7O
Purity: ≥ 98%
CAS#: 1229236-86-5
Solubility: DMSO up to 100 mM
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
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LY2784544 is highly potent and selective mutant JAK2 (V617F) inhibitor with an IC50 of ~55 nM. It also inhibits IL-3-activated wild type JAK2 with an IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows anti-proliferative activity in JAK2 V617F-driven cells with an IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. LY2784544 significantly inhibits STAT5 phosphorylation in JAK2-V617F Ba/F3 xenografts. Currently LY2784544 is being investigated in a clinical trial for the treatment of essential thrombocythemia, polycythemia vera, and primary myelofibrosis.

 

How to Use:

  • In vitro:  LY2784544 was used at 5-10 µM final concentration in vitro and in cellular assays.
  • In vivo:  LY2784544 significantly inhibits STAT5 phosphorylation in JAK2-V617F Ba/F3 xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces JAK2-V617F Ba/F3 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.

 

Reference:

  • 1. Srdan Verstovsek . Phase I Study of the JAK2 V617F Inhibitor, LY2784544, in Patients with Myelofibrosis (MF), Polycythemia Vera (PV), and Essential Thrombocythemia (ET). (2011) 53rd ASH Annual Meeting and Exposition.
  • 2. Liandong Ma. Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models. (2011) 53rd ASH Annual Meeting and Exposition.
  • 3. David Mitchell, et al. Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544. (2012) Org. Process Res. Dev., 16 (1), pp 70–81

 

LY2784544_spec.pdf

LY2784544_MSDS.pdf

 

Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 469.94
Formula: C23H25ClFN7O
Purity: ≥ 98%
CAS#: 1229236-86-5
Solubility: DMSO up to 100 mM
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
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

LY2784544 is highly potent and selective mutant JAK2 (V617F) inhibitor with an IC50 of ~55 nM. It also inhibits IL-3-activated wild type JAK2 with an IC50 of 2.26 μM. Similarly in the proliferation assay, LY2784544 shows anti-proliferative activity in JAK2 V617F-driven cells with an IC50 of 68 nM, compared to 1.36 μM in wild type JAK2-driven cells and 0.94 μM in JAK3-driven cells. LY2784544 significantly inhibits STAT5 phosphorylation in JAK2-V617F Ba/F3 xenografts. Currently LY2784544 is being investigated in a clinical trial for the treatment of essential thrombocythemia, polycythemia vera, and primary myelofibrosis.

 

How to Use:

  • In vitro:  LY2784544 was used at 5-10 µM final concentration in vitro and in cellular assays.
  • In vivo:  LY2784544 significantly inhibits STAT5 phosphorylation in JAK2-V617F Ba/F3 xenografts with a Threshold Effective Dose 50 (TED50) of 12.7 mg/kg. LY2784544 also reduces JAK2-V617F Ba/F3 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.

 

Reference:

  • 1. Srdan Verstovsek . Phase I Study of the JAK2 V617F Inhibitor, LY2784544, in Patients with Myelofibrosis (MF), Polycythemia Vera (PV), and Essential Thrombocythemia (ET). (2011) 53rd ASH Annual Meeting and Exposition.
  • 2. Liandong Ma. Efficacy of LY2784544, a Small Molecule Inhibitor Selective for Mutant JAK2 Kinase, In JAK2 V617F-Induced Hematologic Malignancy Models. (2011) 53rd ASH Annual Meeting and Exposition.
  • 3. David Mitchell, et al. Development and a Practical Synthesis of the JAK2 Inhibitor LY2784544. (2012) Org. Process Res. Dev., 16 (1), pp 70–81

 

LY2784544_spec.pdf

LY2784544_MSDS.pdf

 

Products are for research use only. Not for human use.

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