GDC-0994

ERK1/2 inhibitor CAS# 1453848-26-4

GDC-0994

Catalog No. BCC6371----Order now to get a substantial discount!

Product Name & Size Price Stock
GDC-0994: 5mg $115 In Stock
GDC-0994: 10mg Please Inquire In Stock
GDC-0994: 20mg Please Inquire Please Inquire
GDC-0994: 50mg Please Inquire Please Inquire
GDC-0994: 100mg Please Inquire Please Inquire
GDC-0994: 200mg Please Inquire Please Inquire
GDC-0994: 500mg Please Inquire Please Inquire
GDC-0994: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of GDC-0994

Number of papers citing our products

Chemical structure

GDC-0994

3D structure

Chemical Properties of GDC-0994

Cas No. 1453848-26-4 SDF Download SDF
PubChem ID 71727581 Appearance Powder
Formula C21H18ClFN6O2 M.Wt 440.86
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Ravoxertinib
Solubility DMSO : ≥ 35 mg/mL (79.39 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one
SMILES CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)C(CO)C4=CC(=C(C=C4)Cl)F
Standard InChIKey RZUOCXOYPYGSKL-GOSISDBHSA-N
Standard InChI InChI=1S/C21H18ClFN6O2/c1-28-19(5-8-25-28)27-21-24-7-4-17(26-21)13-6-9-29(20(31)11-13)18(12-30)14-2-3-15(22)16(23)10-14/h2-11,18,30H,12H2,1H3,(H,24,26,27)/t18-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GDC-0994

DescriptionGDC-0994 is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.In Vitro:GDC-0994 also inhibits p90RSK with IC50 of 12 nM[1]. GDC-0994 is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2].In Vivo:In CD-1 mice, a 10 mg/kg oral dose of GDC-0994 is sufficient to achieve the desired target coverage for at least 8 h[1]. Daily, oral dosing of GDC-0994 results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice[2].

References:
[1]. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme [2]. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.

Protocol

Animal Administration [1]
Mice[1] PK/PD data for GDC-0994 in the HCT116 mouse xenograft model. HCT116 tumors are established in nude mice to a tumor volume of 400−600 mm3. Mice are treated with a single oral dose of 22 at 15, 30, or 100 mg/kg versus vehicle control alone (40% PEG400/60% (10% HPβCD)) follow by tumor and plasma collection at 2, 8, 16, and 24 h postdose. Tumor levels of phosphorylated p90RSK (pRSK) relative total p90RSK (tRSK) are measured by quantitative Western blot and are normalized to vehicle control at 2 h postdose (set to 100%). Plasma and tumor concentrations are measured by LC−MS.

References:
[1]. Blake JF, et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Developme [2]. Kirk Robarge, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. Proceedings: AACR Annual Meeting 2014; April 5-9, 2014.

GDC-0994 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

GDC-0994 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of GDC-0994

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2683 mL 11.3415 mL 22.6829 mL 45.3659 mL 56.7073 mL
5 mM 0.4537 mL 2.2683 mL 4.5366 mL 9.0732 mL 11.3415 mL
10 mM 0.2268 mL 1.1341 mL 2.2683 mL 4.5366 mL 5.6707 mL
50 mM 0.0454 mL 0.2268 mL 0.4537 mL 0.9073 mL 1.1341 mL
100 mM 0.0227 mL 0.1134 mL 0.2268 mL 0.4537 mL 0.5671 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on GDC-0994

GDC-0994 is a potent and selective inhibitor of ERK1/2 with IC50 values of 1.1 and 0.3 nM, respectively [1].

The extracellular-signal-regulated kinases (ERK1 and ERK2) are members of the MAP kinase family and act downstream of the RAS/RAF/MEK/ERK signaling cascade that are commonly activated by upstream oncogenic signaling or oncogenic mutations in BRAF or RAS. ERK1/2 play important roles in proliferation, differentiation and cell cycle progression [1].

GDC-0994 is an orally available and potent ERK1/2 inhibitor with potential antineoplastic activity. In mice bearing KRAS-mutant and BRAF-mutant human xenograft tumors, GDC-0994 exhibited significant single-agent activity and inhibited phospho-p90RSK [1]. When orally administration, GDC-0994 inhibited both activation of ERK-mediated signal transduction pathways and ERK phosphorylation, which then inhibited ERK-dependent tumor cell survival and proliferation.

References:
[1].  Robarge K, Schwarz J, Blake J, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. AACR Annual Meeting, 2014, San Diego, CA.

Featured Products
New Products
 

References on GDC-0994

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-y l)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.[Pubmed:27227380]

J Med Chem. 2016 Jun 23;59(12):5650-60.

The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream nodes with RAF and MEK inhibitors has proven effective clinically, resistance frequently develops through reactivation of the pathway. Simultaneous targeting of multiple nodes in the pathway, such as MEK and ERK, offers the prospect of enhanced efficacy as well as reduced potential for acquired resistance. Described herein is the discovery and characterization of GDC-0994 (22), an orally bioavailable small molecule inhibitor selective for ERK kinase activity.

Description

Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

Keywords:

GDC-0994,1453848-26-4,Ravoxertinib,Natural Products,MEK1/2, buy GDC-0994 , GDC-0994 supplier , purchase GDC-0994 , GDC-0994 cost , GDC-0994 manufacturer , order GDC-0994 , high purity GDC-0994

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: