1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

LY3214996 

Cat. No.: HY-101494 Purity: 99.87%
Handling Instructions

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

For research use only. We do not sell to patients.

LY3214996 Chemical Structure

LY3214996 Chemical Structure

CAS No. : 1951483-29-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 239 In-stock
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 380 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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View All ERK Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target[1]

ERK1

5 nM (IC50)

ERK2

5 nM (IC50)

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 inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. LY3214996 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 LY3214996 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, LY3214996 can be tailored for treatment of cancers with MAPK pathway alteration. In addition, LY3214996 has anti-tumor activity in a Vemurafenib-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, LY3214996 can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of LY3214996 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 15 mg/mL (33.07 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2048 mL 11.0239 mL 22.0478 mL
5 mM 0.4410 mL 2.2048 mL 4.4096 mL
10 mM 0.2205 mL 1.1024 mL 2.2048 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

453.56

Formula

C₂₂H₂₇N₇O₂S

CAS No.

1951483-29-6

SMILES

O=C(C(C=C(C1=NC(NC2=CC=NN2C)=NC=C1)S3)=C3C4(C)C)N4CCN5CCOCC5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LY3214996
Cat. No.:
HY-101494
Quantity:

LY3214996

Cat. No.: HY-101494