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Ralimetinib

Cat. No. M30721

All AbMole products are for research use only, cannot be used for human consumption.

Ralimetinib Structure
Synonym:

LY2228820

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Quality Control & Documentation
Biological Activity

Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

Chemical Information
Molecular Weight 420.53
Formula C24H29FN6
CAS Number 862505-00-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
References

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

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

[3] Ignace Vergote, et al. Gynecol Oncol. A randomized, double-blind, placebo-controlled phase 1b/2 study of ralimetinib, a p38 MAPK inhibitor, plus gemcitabine and carboplatin versus gemcitabine and carboplatin for women with recurrent platinum-sensitive ovarian cancer

[4] Johanna C Bendell, et al. Invest New Drugs. A phase 1 dose-escalation study of checkpoint kinase 1 (CHK1) inhibitor prexasertib in combination with p38 mitogen-activated protein kinase (p38 MAPK) inhibitor ralimetinib in patients with advanced or metastatic cancer

[5] Amita Patnaik, et al. Clin Cancer Res. A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients with Advanced Cancer

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Keywords: Ralimetinib, LY2228820 supplier, p38 MAPK, inhibitors, activators

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