ChemicalBook > CAS DataBase List > LY2228820

LY2228820

Product Name: LY2228820
CAS No.: 862507-23-1
Chemical Name: LY2228820
Synonyms: CS-371;LY2228820;LY2228820 2MsOH;Ralimetinib 2MsOH;LY2228820 USP/EP/BP;LY2228820 diMesylate;LY2228820 (mesylate);Ralimetinib Mesylate;LY2228820(LY-2228820);LY2228820 (Ralimetinib)
CBNumber: CB82518277
Molecular Formula: C26H37FN6O6S2
Formula Weight: 612.7369832
MOL File: 862507-23-1.mol

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LY2228820 Property

storage temp.: Store at -20°C
solubility: ≥30.65 mg/mL in DMSO; ≥45 mg/mL in H2O with ultrasonic; ≥9.9 mg/mL in EtOH with ultrasonic
form: solid
color: White to yellow
InChIKey: CQTHGFJRTIZYQG-UHFFFAOYSA-N
SMILES: C12N(CC(C)(C)C)C(N)=NC1=CC=C(C1NC(C(C)(C)C)=NC=1C1=CC=C(F)C=C1)N=2.CS(O)(=O)=O

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Safety

HS Code: 2933998090

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23259
Product name: LY2228820 (mesylate)
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23259
Product name: LY2228820 (mesylate)
Purity: ≥98%
Packaging: 5mg
Price: $145
Updated: 2024/03/01

Cayman Chemical

Product number: 23259
Product name: LY2228820 (mesylate)
Purity: ≥98%
Packaging: 10mg
Price: $275
Updated: 2024/03/01

Cayman Chemical

Product number: 23259
Product name: LY2228820 (mesylate)
Purity: ≥98%
Packaging: 25mg
Price: $571
Updated: 2024/03/01

Usbiological

Product number: 281305
Product name: LY2228820
Packaging: 2mg
Price: $495
Updated: 2021/12/16

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LY2228820 Chemical Properties,Usage,Production

Uses

LY2228820 is a novel and potent p38MAPK inhibitor with potent antiinflammatory activity. LY2228820 significantly inhibited phosphorylation of MAPKAPK2 and/or HSP27, down stream targets of p38MAPK, in both multiple myeloma (MM) cell lines and LT-BMSCs. LY2228820 is a potential candidate to improve MM patient outcome both by enhancing the effect of Bortezomib (B675700) and by reducing osteoskeletal events.

Biological Activity

ly2228820 is a potent, selective, atp-competitive small-molecule inhibitor inhibiting α- and β-isoforms of p38 mapk with ic(50) values of 5.3nm and 3.2 nm, respectively1.in multiple myeloma (mm) cell lines, ly2228820 enhanced the cytotoxicity of bortezomiba via reducing bortezomib-induced phosphorylation of heat shock protein 27 (hsp27). ly2228820 significantly reduced il-6 secretion from bm mononuclear cells (bmmncs) and long term cultured-bm stromal cells (lt-bmscs). besides, ly2228820 can also inhibit secretion of macrophage inflammatory protein-1a (mip-1a) in bmmncs, cd138+ patient mm cells and normal cd14+ osteoclast cells 2.studies in mice implanted with b16-f10 melanoma showed that orally administered ly2228820 can effectively suppress the tumor-phospho-mk2 expression. treatment of ly2228820 caused a significant tumor growth delay in a549 nsclc xenograft models1.

in vivo

In LPS-induced mice, Ralimetinib dimesylate effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED₅₀) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), Ralimetinib dimesylate displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED₅₀)of 1.5 mg/kg^[1]. Ralimetinib dimesylate inhibits tumor phospho-MK2 in a dose-dependent manner (TED₅₀=1.95 mg/kg, TED₇₀=11.17 mg/kg) in mice implanted with B16-F10 melanoma. Ralimetinib dimesylate inhibits MK2 phosphorylation: mouse in vivo TED₅₀=1.01 mg/kg (compound exposure approximately 100 nM) and human ex vivo IC₅₀=0.12 μM with either mouse or human PBMC^[3].

target

p38α

IC 50

p38β MAPK: 3.2 nM (IC₅₀); p38α MAPK: 5.3 nM (IC₅₀)

References

1. campbell rm1, anderson bd, brooks na, brooks hb, chan em, de dios a, gilmour r, graff jr, jambrina e, mader m, mccann d, na s, parsons sh, pratt se, shih c, stancato lf, starling jj, tate c, velasco ja, wang y, ye xs.characterization of ly2228820 dimesylate, a potent and selective inhibitor of p38 mapk with antitumor activity. mol cancer ther. 2014 feb;13(2):364-74.2. ishitsuka k1, hideshima t, neri p, vallet s, shiraishi n, okawa y, shen z, raje n, kiziltepe t, ocio em, chauhan d, tassone p, munshi n, campbell rm, dios ad, shih c, starling jj, tamura k, anderson kc. p38 mitogen-activated protein kinase inhibitor ly2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. br j haematol. 2008 may;141(5):598-606.

LY2228820 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from LY2228820 manufacturers

Career Henan Chemical Co

Product: LY2228820 862507-23-1
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 200kg
Release date: 2020-01-10

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LY2228820;LY 2228820;LY-2228820

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LY2228820(LY-2228820)

LY2228820 2MsOH

LY2228820 diMesylate

5-[2-(tert-Butyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)-3H-imidazo[4,5-b]pyridin-2-amine methanesulfonate

LY2228820 (Ralimetinib) dimesylate

LY2228820 (mesylate)

Ralimetinib Mesylate

RALIMETINIB DIMESYLATE (LY2228820 DIMESYLATE)

Ralimetinib 2MsOH(LY2228820)

CS-371

LY2228820 (Ralimetinib)

RALIMETINIB DIMESYLATE; LY2228820 DIMESYLATE; LY2228820 2MSOH; LY 2228820; LY-2228820

Ralimetinib 2MsOH

LY2228820 USP/EP/BP

Ralimetinib dimysylate (LY2228820 dimysylate)

Ralimetinib mesylate LY2228820 LY-2228820

LY 2228820, p38 MAPK inhibitor

Ralimetinib dimesylate, 10 mM in DMSO

LY2228820 dimesylate (Ralimetinib dimesylate)

Ralimetinib (LY2228820) dimesylate

Ralimetinib (LY2228820) dimesylate ，S1494

862507-23-1

C24H29FN62CH4O3S

C25H33FN6O3S

C26H37FN6O6S2

MAPK

Inhibitors

Aromatics

Heterocycles

Intermediates & Fine Chemicals

Pharmaceuticals

Protein Kinase Inhibitors and Activators