ChemicalBook > CAS DataBase List > GDC-0994

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

Less

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

Less

Safety

HS Code: 2933998090

Less

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.

Less

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

Less

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

Less

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: 16077
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

SINO High Goal Chemical Technology Co., Ltd.

Tel: 021-57646680 18306277365
Fax: 2469917557
Email: sunkai@chembiobanksh.com
Country: China
ProdList: 2040
Advantage: 55

DONGSHENG CHIRAL PHARMA

Tel: 15800326364 18051538752
Email: 582512789@qq.com
Country: China
ProdList: 449
Advantage: 55

AdooQ Bioscience CHINA

Tel: 025-58849295 18951903616;
Fax: 025-68650336
Email: info@adooq.cn
Country: China
ProdList: 2990
Advantage: 60

LETOPHARM LIMITED

Tel: +86-21-5821 5861
Fax: +86-21-5106 2861
Email: sales@letopharm.com
Country: China
ProdList: 2384
Advantage: 58

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4768
Advantage: 55

Wuhan ChemFaces Biochemical Co., Ltd.

Tel: 18607101326 15172504745
Fax: +86-27-84254680
Email: aileen@chemfaces.com
Country: China
ProdList: 6905
Advantage: 55

Guangzhou QiYun Biotechnology Co., Ltd.

Tel: 020-61288194 61288195
Fax: 020-61288700
Email: 505721671@qq.com
Country: China
ProdList: 3866
Advantage: 58

parabiochem

Tel: 025-83453382-8005
Fax: 025-83453382
Email: sale@parabiochem.com
Country: China
ProdList: 9595
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
Advantage: 62

Shanghai Rechem science Co., Ltd.

Tel: 021-31433387 15618786686
Fax: QQ:1369748377
Email: sales@rechemscience.com
Country: China
ProdList: 2991
Advantage: 58

Jinan elephant international trading co., LTD

Tel
Fax: -
Email: 13006575422@163.com
Country: China
ProdList: 6355
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9125
Advantage: 58

Beijing Solarbio Science & Tecnology Co., Ltd.

Tel: 010-50973130 18101056239
Email: 3193328036@qq.com
Country: China
ProdList: 29759
Advantage: 68

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
Advantage: 58

Zhongshan Geometric Biological Technology Co., Ltd.

Tel
Email: 2953972351@qq.com
Country: China
ProdList: 253
Advantage: 58

Medi-tech Bioscientific Co., Ltd.

Tel: 0519-83246372 13585352506
Fax: 0519-83246372
Country: China
ProdList: 1844
Advantage: 58

Kaixin Chemical (Hong Kong) Limited

Tel: 010-88886666-01 13112345678
Fax: CDXH21@126.com
Email: loyson@tcypharm.com
Country: China
ProdList: 597
Advantage: 55

Nanjing Nohon Biological Technology Co., Ltd.

Tel: 025-85767923 18512596075
Fax: 025-85767923
Email: sales@nuoxibio.com
Country: China
ProdList: 962
Advantage: 55

Dezhou LonWel Pharmaceutical Technology Co., Ltd.

Tel: 13761310616
Fax: QQ: 39324283
Email: 39324283@qq.com
Country: China
ProdList: 1628
Advantage: 58

Shanghai Biopharmaleader Co., Ltd.

Tel: +86 18721201413
Fax: +86 (21) 5775-8967
Email: sales@biopharmaleader.com
Country: China
ProdList: 1720
Advantage: 58

Jiaxing Deyi Chemical Co., Ltd.

Tel: 86-0573-85866609 13325730825
Fax: 0573-85866609
Email: 945717149@qq.com
Country: China
ProdList: 8595
Advantage: 58

Shanghai Benso Pharmaceutical Technology Co., Ltd.

Tel: 15088289376
Email: 248775804@qq.com
Country: China
ProdList: 4995
Advantage: 58

Angel Pharmatech, Ltd.

Tel: 17317130613
Fax: QQ3358272972
Email: 3358272972@qq.com
Country: China
ProdList: 3277
Advantage: 58

Beijing OKA biological technology co., LTD

Tel: 010-62971590 18548936886
Fax: 010-62340519
Email: 3462612863@qq.com
Country: China
ProdList: 10063
Advantage: 58

Shanghai Medicil Biomedical Co., Ltd.

Tel: 021-50822001
Email: marketing@medicilon.com.cn
Country: China
ProdList: 1152
Advantage: 58

Fan De(Beijing) Biotechnology Co., Ltd.

Tel: 15911056312
Email: liming@bio-fount.com
Country: China
ProdList: 9729
Advantage: 58

Guangzhou Tomums Life Science Co., Ltd.

Tel: 020-31155029 18902330969
Fax: 020-31155029
Email: sales@tomums.cn
Country: China
ProdList: 4696
Advantage: 58

Ningbo Haorui Biological Technology Co., Ltd.

Tel: 15221000252
Email: 843015720@qq.com
Country: CHINA
ProdList: 65
Advantage: 58

Taizhou Crene Biotechnology Co. Ltd.

Tel: +86-0576-88813233 +86-13396860566
Email: sales@pharm-intermediates.com
Country: China
ProdList: 1991
Advantage: 58

Shanghai zhigan biotechnology co., LTD

Tel
Email: zhiqianbio@126.com
Country: China
ProdList: 19778
Advantage: 58

Allfluoro pharmaceutical co. ltd.

Tel: +86-400-0216110 +86-15958047586
Fax: 0086-21-33275002
Email: sales@allfluoro.com
Country: China
ProdList: 11385
Advantage: 58

HANGZHOU CLAP TECHNOLOGY CO.,LTD

Tel: 86-571-88216897,88216896 13588875226
Fax: 86-571-88216895
Email: sales@hzclap.com
Country: CHINA
ProdList: 6312
Advantage: 58

HaBo Hong Kong Co., Limited.

Tel: +86-25-18512596065
Email: info@habotech.com
Country: CHINA
ProdList: 933
Advantage: 58

Ningbo Haorui Biological Technology Co., Ltd.

Tel: 15221000252
Email: 278450236@qq.com
Country: China
ProdList: 203
Advantage: 58

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: +86-0519-85788828 +86-13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3934
Advantage: 58

Shanghai jingkang bioengineering co., ltd.

Tel: 021-54721350 13524668266
Fax: 021-5
Email: 2881505714@qq.com
Country: China
ProdList: 7872
Advantage: 58

career henan chemical co

Tel: +86-0371-86658258 +8613203830695
Fax: 0086-371-86658258
Email: factory@coreychem.com
Country: China
ProdList: 29798
Advantage: 58

Shanghai Zeye Biotechnology Co., Ltd.

Tel: 021-021-61998551 13122364865
Email: sale1@shzysw.net
Country: China
ProdList: 9778
Advantage: 58

Absin Bioscience Inc.

Tel: 021-38015121 18438616290
Email: lanwu@univ-bio.com
Country: China
ProdList: 24731
Advantage: 58

Shanghai hongqu biomedical technology co. LTD

Tel: 88888888888
Email: hongquchem@qq.com
Country: China
ProdList: 5132
Advantage: 58

Shanghai Luofa Biochemical Technology Co., Ltd.

Tel: 021-51111890 15317326293
Email: sales@molnova.com
Country: China
ProdList: 4195
Advantage: 58

Advanced chemblocks inc

Tel: 650-6922368
Email: sales@achemblock.com
Country: China
ProdList: 2992
Advantage: 58

Less

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