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Temuterkib

Catalog No. T4091 CAS 1951483-29-6

Synonyms: LY3214996

Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.

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Temuterkib, CAS 1951483-29-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 64.00
2 mg	In stock	$ 84.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 427.00
50 mg	In stock	$ 646.00
100 mg	In stock	$ 919.00
500 mg	In stock	$ 1,860.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.57%

Purity: 99.37%

Biological Description

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Description	Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity.
Targets&IC50	ERK2:5 nM, ERK1:5 nM
In vitro	LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. LY3214996 potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to LY3214996[1].
In vivo	In tumor xenograft models, LY3214996 effectively inhibits the PD biomarker phospho-p90RSK1 and its PD effects, correlating with compound exposure and antitumor activity. It demonstrates comparable or superior efficacy to existing ERK inhibitors in BRAF or RAS mutant cell lines and xenografts. Oral administration of LY3214996 notably suppresses tumor growth across various cancer xenografts, including BRAF or NRAS mutant melanoma, and BRAF or KRAS mutant colorectal, lung, and pancreatic cancers, showing good tolerance. It offers a promising therapeutic strategy for cancers linked to MAPK pathway alterations. Remarkably, LY3214996 also counters Vemurafenib-resistant A375 melanoma xenografts, highlighting its potential in treating melanoma patients unresponsive to BRAF therapy. Furthermore, LY3214996 can be used alongside investigational and approved treatments, especially in KRAS mutant cases. Its combination with the CDK4/6 inhibitor abemaciclib exhibits significant tumor growth inhibition or regression in diverse cancer models, including KRAS mutant colorectal and non-small cell lung cancers, showcasing its broad therapeutic potential[1].

Synonyms	LY3214996
Molecular Weight	453.56
Formula	C22H27N7O2S
CAS No.	1951483-29-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (26.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Shripad V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Research. July 2017. 2. Li X, Qin X, Tian J, et al. Liquiritin protects PC12 cells from corticosterone-induced neurotoxicity via regulation of metabolic disorders, attenuation ERK1/2-NF-κB pathway, activation Nrf2-Keap1 pathway, and inhibition mitochondrial apoptosis pathway[J]. Food and Chemical Toxicology. 2020: 111801.

Citations

1. Li X, Qin X, Tian J, et al. Liquiritin protects PC12 cells from corticosterone-induced neurotoxicity via regulation of metabolic disorders, attenuation ERK1/2-NF-κB pathway, activation Nrf2-Keap1 pathway, and inhibition mitochondrial apoptosis pathway. Food and Chemical Toxicology. 2020: 111801 2. Chen S J, Huang Y, Yu F, et al.BMAL1/p53 mediating bronchial epithelial cell autophagy contributes to PM2. 5-aggravated asthma.Cell Communication and Signaling.2023, 21(1): 39.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Kinase Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-Cancer Clinical Compound Library Stem Cell Differentiation Compound Library Clinical Compound Library Anti-Ovarian Cancer Compound Library

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Keywords

Temuterkib 1951483-29-6 MAPK ERK inhibit Extracellular signal regulated kinases LY-3214996 LY 3214996 LY3214996 Inhibitor inhibitor

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