GDC-0853

Product Name: GDC-0853
CAS No.: 1434048-34-6
Chemical Name: GDC-0853
Synonyms: GDC0853;CS-2241;EOS-61209;FENEBRUTINIB;GDC-0853;GDC 0853;GDC-0853 (RG7845);GDC-0853/Fenebrutinib;FENEBRUTINIB (GDC-0853);Fenebrutinib, 10 mM in DMSO;inhibit,Inhibitor,GDC0853,GDC 0853,Fenebrutinib,Btk,Bruton tyrosine kinase
CBNumber: CB33142405
Molecular Formula: C37H44N8O4
Formula Weight: 664.8
MOL File: 1434048-34-6.mol

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GDC-0853 Property

Boiling point:: 936.3±65.0 °C(Predicted)
Density: 1.42±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMF:20.0(Max Conc. mg/mL);30.08(Max Conc. mM)
DMSO:17.0(Max Conc. mg/mL);25.57(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.5(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);7.52(Max Conc. mM)
form: A crystalline solid
pka: 13.15±0.10(Predicted)
color: White to off-white
InChIKey: WNEODWDFDXWOLU-QHCPKHFHSA-N
SMILES: C12=CC3CC(C)(C)CC=3N1CCN(C1=NC=CC(C3C=C(NC4=NC=C(N5CCN(C6COC6)C[C@@H]5C)C=C4)C(=O)N(C)C=3)=C1CO)C2=O

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 21346
Product name: GDC-0853
Purity: ≥98%
Packaging: 1mg
Price: $39
Updated: 2024/03/01

Cayman Chemical

Product number: 21346
Product name: GDC-0853
Purity: ≥98%
Packaging: 5mg
Price: $180
Updated: 2024/03/01

Cayman Chemical

Product number: 21346
Product name: GDC-0853
Purity: ≥98%
Packaging: 10mg
Price: $340
Updated: 2024/03/01

Cayman Chemical

Product number: 21346
Product name: GDC-0853
Purity: ≥98%
Packaging: 25mg
Price: $647
Updated: 2023/06/20

TRC

Product number: F247550
Product name: Fenebrutinib
Packaging: 5mg
Price: $440
Updated: 2021/12/16

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GDC-0853 Chemical Properties,Usage,Production

Description

GDC-0853 is an orally bioavailable, selective, and reversible Bruton’s tyrosine kinase (BTK) inhibitor with IC₅₀s ranging from 2-9 nM for basophil activation, B cell receptor activation, and constitutive p-BTK activity in whole blood lysates. In rats, treatment for longer than 7 days leads to pancreatic toxicity but it does not occur in mice or dogs, even at higher doses. Formulations containing GDC-0853 were well-tolerated in Phase I clinical trials and are in additional clinical trials for rheumatoid arthritis, lupus erythematosus, lymphoma, and leukemia.

Uses

Fenebrutinib is a selective and reversible oral small-molecular BTK inhibitor for the treatment of rheumatoid arthritis and systemic lupus erythematosus.

in vivo

Fenebrutinib (GDC-0853) dose-dependently reduces ankle thickness following once (0.06, 0.25, 1, 4, and 16 mg/kg QD; orally) or twice (0.125, 0.5, and 2 mg/kg BID; orally) daily in female Lewis rats with developing collagen-induced arthritis^[2].
Fenebrutinib (0.2 mg/kg IV and 1.0 mg/kg PO; for rats) and (0.2 mg/kg IV and 0.5 mg/kg PO for dogs) demonstrates the half-lives (t_1/2s) of 2.2 and 3.8 h In rats, and dogs, respectively^[2].

Animal Model:	Female Lewis rats with developing collagen-induced arthritis (CIA)^[2]
Dosage:	0.06, 0.25, 1, 4, and 16 mg/kg once daily (QD); 0.125, 0.5, and 2 mg/kg twice daily (BID)
Administration:	Dosed orally; for 16 days
Result:	Dose-dependently reduced ankle thickness following QD and BID dosing regimens.

References

[1] JAMES J. CRAWFORD*. Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development[J]. Journal of Medicinal Chemistry, 2018, 61 6: 2227-2245. DOI: 10.1021/acs.jmedchem.7b01712

GDC-0853 Preparation Products And Raw materials

Raw materials

Preparation Products

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GDC-0853 Suppliers

China 89 India 2 United States 9 Global 100

Nantong Hanfang Biotechnology Co. , Ltd.

Tel: hanfangpharma@126.com; 18616537568
Email: hanfangpharma@126.com
Country: China
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Shanghai XingMo Biotechnology Co., Ltd.

Tel: +86 13524779951; 13524779951
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Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070
Fax: +86-25-83453306
Email: info@chemlin.com.cn
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Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
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Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
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MedChemexpress LLC

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Country: United States
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Shanghai Lollane Biological Technology Co.,Ltd.

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Shanghaizehan biopharma technology co., Ltd.

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Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
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Cangzhou Enke Pharma-tech Co., Ltd.

Tel: 0317-5296180 15533709196
Fax: 0317-5106596
Email: sale@enkepharma.com
Country: China
ProdList: 2247
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View Lastest Price from GDC-0853 manufacturers

Career Henan Chemical Co

Product: GDC-0853 1434048-34-6
Price: US $6.68/KG
Min. Order: 1KG
Purity: 97%-99%
Supply Ability: 1kg-1000kg
Release date: 2020-01-08

1434048-34-6, GDC-0853Related Search:

(S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one

GDC0853

EOS-61209

GDC-0853 (RG7845)

GDC-0853;GDC 0853

FENEBRUTINIB (GDC-0853)

FENEBRUTINIB

CS-2241

GDC-0853/Fenebrutinib

2H-Cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one, 2-[1,6-dihydro-3'-(hydroxymethyl)-1-methyl-5-[[5-[(2S)-2-methyl-4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-oxo[3,4'-bipyridin]-2'-yl]-3,4,7,8-tetrahydro-7,7-dimethyl-

2-[1,6-Dihydro-3'-(hydroxymethyl)-1-methyl-5-[[5-[(2S)-2-methyl-4-(3-oxetanyl)-1-piperazinyl]-2-pyridinyl]amino]-6-oxo[3,4'-bipyridin]-2'-yl]-3,4,7,8-tetrahydro-7,7-dimethyl-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one

inhibit,Inhibitor,GDC0853,GDC 0853,Fenebrutinib,Btk,Bruton tyrosine kinase

2-1,6-Dihydro-3'-(hydroxymethyl)-1-methyl-5-5-(2S)-2-methyl-4-(3-oxetanyl)piperazin-1-ylpyridin-2-ylamino-6-oxo3,4'-bipyridin-2'-yl-3,4,7,8-tetrahydro-7,7-dimethyl-2H-cyclopenta4,5pyrrolo1,2-apyrazin-1(6H)-one

(S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one

Fenebrutinib, 10 mM in DMSO

(S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one

1434048-34-6