Free shipping on all orders over $ 500

LY2784544

Cat. No. M3535
LY2784544 Structure
Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 200 In stock
50mg USD 650 In stock
Bulk Inquiry?

Quality Control
Biological Activity

LY2784544 is a small molecule selective mutant JAK2 kinase inhibitor with an IC50 of 68 nM. The antiproliferative activity of LY2784544 and its ability to induce apoptosis were examined by Celltiter-Glo Cell Viability and Caspase-Glo 3/7 Apoptosis Assays, respectively.? In the in vitro tests using Ba/F3 cells expressing either wild type or V617F mutant JAK2, it potently inhibited the JAK2 V617F-STAT5 signaling at a concentration that was 41-fold lower than that required to inhibit IL-3-activated wild type JAK2-STAT5 signaling (IC50 = 0.055 uM for JAK2 V617F vs. 2.26 uM for WT JAK2). Similarly in the proliferation assay, LY2784544 selectively inhibited the JAK2 V617F-driven cell proliferation (IC50= 0.068 uM). Inhibition of JAK2 V617F signaling correlated well with the induction of apoptosis (EC50= 0.113 uM) in Ba/F3 cell model.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 469.94
Formula C23H25ClFN7O
CAS Number 1229236-86-5
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
Related JAK Products
Ruxolitinib phosphate

Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.

Oclacitinib maleate

Oclacitinib is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases.

Baricitinib phosphate

Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.

JANEX-1

Janex-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 μM); has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases.

Decernotinib

Decernotinib is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2784544 supplier, JAK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.