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LY2228820

Cat. No. M2318
LY2228820 Structure
Synonym:

Ralimetinib dimesylate; LY2228820 dimesylate; LY2228820 2MsOH

Size Price Availability Quantity
2mg USD 60  USD60 In stock
5mg USD 95  USD95 In stock
10mg USD 160  USD160 In stock
50mg USD 580  USD580 In stock
100mg USD 950  USD950 In stock
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Quality Control & Documentation
Biological Activity

LY2228820 is a novel and potent p38MAPK inhibitor. In vitro kinase enzyme activity showed that the IC50 for p38αMAPK and p38βMAPK of LY2228820 were 7 nM and 3 nM, respectively. Phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, was significantly inhibited by LY in both MM cell lines and LT-BMSCs.

Customer Product Validations & Biological Datas
Source Oncotarget (2016). Figure 3. LY2228820
Method colony assays
Cell Lines MDA-MB-231 cells
Concentrations 10 μM
Incubation Time 72 h
Results The triple combination significantly retarded shortterm proliferation of MDA-MB-231 cells compared to vehicle and single drug controls (p<0.001), as well as the two-agent combinations
Chemical Information
Molecular Weight 612.74
Formula C24H29FN6.2CH4O3S
CAS Number 862507-23-1
Solubility (25°C) DMSO 20 mg/mL
Water 83 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Ann-Kathrin Reuschl, et al. Host-directed therapies against early-lineage SARS-CoV-2 retain efficacy against B.1.1.7 variant

[2] J Biau, et al. Phase 1 trial of ralimetinib (LY2228820) with radiotherapy plus concomitant temozolomide in the treatment of newly diagnosed glioblastoma

[3] Jian Wang, et al. CDK7 inhibitor THZ1 enhances antiPD-1 therapy efficacy via the p38α/MYC/PD-L1 signaling in non-small cell lung cancer

[4] Ronggao Chen, et al. LY2228820 induces synergistic anti-cancer effects with anti-microtubule chemotherapeutic agents independent of P-glycoprotein in multidrug resistant cancer cells

[5] Robert M Campbell, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity

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  Catalog
Abmole Inhibitor Catalog




Keywords: LY2228820, Ralimetinib dimesylate; LY2228820 dimesylate; LY2228820 2MsOH supplier, p38 MAPK, inhibitors, activators


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