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GDC-0994

Product Name
GDC-0994
CAS No.
1453848-26-4
Chemical Name
GDC-0994
Synonyms
CS-1841;GDC-0994;RG-7842);EOS-60648;Ravoxertinib;GDC-0994;RAVOXERTINIB;RAVOXERTINIB (GDC-0994);GDC 0994;GDC-0994;GDC0994;Ravoxertinib, 10 mM in DMSO;Ravoxertinib (GDC-0994) ，S7554
CBNumber
CB62716237
Molecular Formula
C21H18ClFN6O2
Formula Weight
440.86
MOL File
1453848-26-4.mol
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GDC-0994 Property

Boiling point:
734.6±70.0 °C(Predicted)
Density 
1.45±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≥44.1 mg/mL in DMSO; insoluble in H2O; ≥19.2 mg/mL in EtOH
form 
solid
pka
14.03±0.10(Predicted)
color 
White to yellow
InChIKey
RZUOCXOYPYGSKL-GOSISDBHSA-N
SMILES
C1(=O)N([C@@H](C2=CC=C(Cl)C(F)=C2)CO)C=CC(C2C=CN=C(NC3N(C)N=CC=3)N=2)=C1
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Safety

HS Code 
2933998090
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21107
Product name
GDC-0994
Purity
≥98%
Packaging
500μg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
21107
Product name
GDC-0994
Purity
≥98%
Packaging
1mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
21107
Product name
GDC-0994
Purity
≥98%
Packaging
5mg
Price
$230
Updated
2024/03/01
Cayman Chemical
Product number
21107
Product name
GDC-0994
Purity
≥98%
Packaging
10mg
Price
$426
Updated
2024/03/01
TRC
Product number
G299910
Product name
GDC-0994
Packaging
2.5mg
Price
$1105
Updated
2021/12/16
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GDC-0994 Chemical Properties,Usage,Production

Description

GDC-0994 is a potent and selective ERK1 and ERK2 inhibitor with IC50 values of 6.1 and 4.1 nM, respectively. It inhibits ERK-dependent p90RSK serine 380 phosphorylation in PMA-stimulated HepG2 cells with an IC50 value of 12 nM. GDC-0994 inhibited growth of HCT116 human colorectal cancer xenograft tumors by 49%, 57%, and 80% at 30, 60, and 100 mg/kg, respectively, when administered orally once daily for 21 days.

Uses

GDC-0994 is a potent and orally available ERK12 inhibitor shown to prevent ERK-dependant tumor cell proliferation and survival.

Synthesis

1453854-96-0

1453848-26-4

Step B: Crude (S)-1-(2-((tert-butyldimethylsilyl)oxy)-1-(4-chloro-3-fluorophenyl)ethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (48 mg) was dissolved in ethyl acetate (4 mL). A solution of ethyl acetate (1.0 mL) saturated with HCl gas was added slowly and dropwise over 2 min. The reaction mixture was stirred at room temperature for 15 min and LCMS analysis showed complete consumption of the raw material. The reaction mixture was concentrated to give an oily residue, which was purified by preparative reversed-phase high-performance liquid chromatography (RP-HPLC) to afford (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 (20.8 mg, 54.6% yield 1H), 7.14 (dd, J = 10.7, 5.1 Hz, 2H), 6.86 (dd, J = 7.3, 1.8 Hz, 1H), 6.27 (d, J = 1.7 Hz, 1H), 5.97 (dd, J = 7.7, 5.7 Hz, 1H), 5.31 (t, J = 5.2 Hz, 1H), 4.15 (m, 1H), 4.10 -3.95 (m, 1H), 3.69 (s, 3H); LCMS m/z 441 (M + H)+.

in vivo

In CD-1 mice, a 10 mg/kg oral dose of Ravoxertinib (GDC-0994) is sufficient to achieve the desired target coverage for at least 8 h[1]. Daily, oral dosing of Ravoxertinib results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice[2].

IC 50

ERK2: 3.1 nM (IC50); ERK1: 6.1 nM (IC50); p-RSK: 12 nM (IC50)

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.

GDC-0994 Preparation Products And Raw materials

Raw materials

Preparation Products

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GDC-0994 Suppliers

China 120 India 1 United States 15 Global 136
Shanghai Changyu Medical Technology Co. Ltd.
Tel
+86-13301875428
Email
sales@changyuhe.com
Country
China
ProdList
311
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
16075
Advantage
64
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4747
Advantage
58
ShangHai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847 13636370518
Fax
021-55068248
Email
shyysw007@163.com
Country
China
ProdList
4999
Advantage
60
Shanghai Topbiochem Technology Co., Ltd
Tel
021-58170097
Email
info@topbiochem.com
Country
China
ProdList
9510
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-6206333 13167063860
Fax
021-50323701
Email
anhua.mao@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
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View Lastest Price from GDC-0994 manufacturers

Career Henan Chemical Co
Product
GDC-0994 1453848-26-4
Price
US $2.00/KG
Min. Order
1g
Purity
98%min
Supply Ability
ask
Release date
2020-01-08

1453848-26-4, GDC-0994Related Search:


  • GDC-0994
  • (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
  • (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
  • 1-[(1S)-1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-2(1H)-pyridinone
  • Ravoxertinib
  • EOS-60648
  • GDC 0994;GDC-0994;GDC0994
  • CS-1841
  • GDC-0994;RAVOXERTINIB
  • RAVOXERTINIB (GDC-0994)
  • 2(1H)-Pyridinone, 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-
  • RG-7842)
  • 1-(1S)-1-(3-Fluoro-4-chlorophenyl)-2-hydroxyethyl-4-2-(1-methyl-1H-pyrazol-5-yl)aminopyrimidin-4-yl-2(1H)-pyridinone
  • GDC-0994 (RAVOXERTINIB, RG7842)
  • Ravoxertinib, 10 mM in DMSO
  • Ravoxertinib (GDC-0994) ，S7554
  • (S)-1-(1-(3-Fluoro-4-chlorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)-pyrimidin-4-yl)-pyridin-2(1H)-one
  • 1453848-26-4
  • C21H18ClFN6O2
  • Inhibitors