BiochemProbe — Life Science Research Reagents

LY3214996 free base · Synonyms: LY-3214996 · LY 3214996

LY3214996 is a highly selective inhibitor of ERK1.

For research use only. Not for human or veterinary use.

Target ERK
Research area Cancer
Purity >98% Stock Inquire
Data Sheet SDS COA

LY3214996 structure

CAS No.: 1951483-29-6

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
50 mg USD 480.00 BP-02137-100mg In stock Get quote
250 mg USD 1,020.00 BP-02137-250mg In stock Get quote
500 mg USD 1,800.00 BP-02137-500mg In stock Get quote
1 g USD 2,850.00 BP-02137-1g In stock Get quote

Need another size or custom synthesis? Request a quote.

Description

LY3214996 is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays.

Biological activity

In Vitro Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib 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 Temuterkib[1]. 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].

Identifiers

SMILES
CN1N=CC=C1NC1=NC=CC(=N1)C1=CC2=C(S1)C(C)(C)N(CCN1CCOCC1)C2=O
InChIKey
JNPRPMBJODOFEC-UHFFFAOYSA-N

Specifications

MW (average)
453.5600
Formula
C22H27N7O2S
CAS No.
1951483-29-6
Physical state
Other
Color
white to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO,>10mg/mL, not in water

Documents

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.

Same target

Search ERK

Same research area

Search Cancer