Basic information Safety Supplier Related

LY3214996

Basic information Safety Supplier Related

LY3214996 Basic information

Product Name:
LY3214996
Synonyms:
  • LY3214996
  • 6,6-dimethyl-2-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)-5-(2-morpholinoethyl)-5,6-dihydro-4H-thieno[2,3-c]pyrrol-4-one
  • CS-2495
  • 4H-Thieno[2,3-c]pyrrol-4-one, 5,6-dihydro-6,6-dimethyl-2-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-5-[2-(4-morpholinyl)ethyl]-
  • Temuterkib
  • Temuterkib (LY3214996)
  • LY-3214996,LY 3214996,inhibit,Extracellular signal regulated kinases,Temuterkib,Inhibitor,ERK
  • LY-3214996 (LY3214996)
CAS:
1951483-29-6
MF:
C22H27N7O2S
MW:
453.56
Mol File:
1951483-29-6.mol
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LY3214996 Chemical Properties

Boiling point:
711.5±70.0 °C(Predicted)
Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:23.5(Max Conc. mg/mL);51.81(Max Conc. mM)
Ethanol:16.0(Max Conc. mg/mL);35.28(Max Conc. mM)
form 
A crystalline solid
pka
6.58±0.10(Predicted)
color 
White to yellow
InChI
InChI=1S/C22H27N7O2S/c1-22(2)19-15(20(30)29(22)9-8-28-10-12-31-13-11-28)14-17(32-19)16-4-6-23-21(25-16)26-18-5-7-24-27(18)3/h4-7,14H,8-13H2,1-3H3,(H,23,25,26)
InChIKey
JNPRPMBJODOFEC-UHFFFAOYSA-N
SMILES
N1(CCN2CCOCC2)C(=O)C2C=C(C3C=CN=C(NC4N(C)N=CC=4)N=3)SC=2C1(C)C
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Safety Information

HS Code 
2934999090
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LY3214996 Usage And Synthesis

Description

LY3214996 is an inhibitor of ERK1 and ERK2 (IC50 = 5 nM for both). It inhibits cell proliferation of tumor cells in vitro, including those expressing B-RAF, N-Ras, or K-Ras mutations. LY3214996 inhibits tumor growth in B-RAF or N-Ras mutant melanoma, B-RAF or K-Ras mutant colorectal, lung, and pancreatic cancer mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models.

Uses

Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.

in vivo

In tumor xenograft models, Temuterkib inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. Temuterkib shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent Temuterkib significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, Temuterkib can be tailored for treatment of cancers with MAPK pathway alteration. In addition, Temuterkib has anti-tumor activity in a PLX4032-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, Temuterkib can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of Temuterkib and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers[1].

IC 50

ERK1: 5 nM (IC50); ERK2: 5 nM (IC50)

References

[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.

LY3214996Supplier

Suzhou Chenrui Biotechnology Co. LTD Gold
Tel
17625585511
Email
1580084073@qq.com
MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
Shanghai Macklin Biochemical Co.,Ltd.
Tel
15221275939
Email
shenlinxing@macklin.cn
Shanghai YuanQi Biotechnology Co., Ltd.
Tel
+86-2332782371 +86-18120098618
Email
sales@adobechem.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
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