R428

Product Name: R428
CAS No.: 1037624-75-1
Chemical Name: R428
Synonyms: R428;BGB-324;CS-1130;EOS-62006;Bemcentinib;BGB324 (R428);R428 (BGB324);R428 USP/EP/BP;BGB-324, CPDB1725;Bemcentinib Crude
CBNumber: CB42621146
Molecular Formula: C30H34N8
Formula Weight: 506.64
MOL File: 1037624-75-1.mol

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R428 Property

Melting point:: >211°C (dec.)
Boiling point:: 799.6±70.0 °C(Predicted)
Density: 1.41±0.1 g/cm3(Predicted)
storage temp.: -20°C
solubility: Soluble in DMSO (up to at least 25 mg/ml)
form: Yellow powder.
pka: 10.34±0.20(Predicted)
color: Yellow
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

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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: 21523
Product name: R428
Purity: ≥98%
Packaging: 1mg
Price: $68
Updated: 2024/03/01

Cayman Chemical

Product number: 21523
Product name: R428
Purity: ≥98%
Packaging: 10mg
Price: $601
Updated: 2024/03/01

Cayman Chemical

Product number: 21523
Product name: R428
Purity: ≥98%
Packaging: 25mg
Price: $1002
Updated: 2024/03/01

TRC

Product number: R060020
Product name: R428
Packaging: 1mg
Price: $50
Updated: 2021/12/16

ApexBio Technology

Product number: A8329
Product name: R428
Packaging: 1mg
Price: $65
Updated: 2021/12/16

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R428 Chemical Properties,Usage,Production

Description

R428 (bemcentinib, BGB324), a selective small-molecule inhibitor of AXL, is currently being evaluated in phase II trials for the treatment of non-small-cell lung cancer (NSCLC) and acute myelocytic leukemia (AML). It has been found to induce apoptosis in cancer cells and to block tumor spread in models of metastatic breast cancer. The therapeutic potential of R428 has also been demonstrated in highly invasive esophageal adenocarcinoma cells and in ESCC cells.
R428 is a selective, small molecule inhibitor of Axl that blocks its catalytic and precancerous activities. R428 treatment reduced Axl-induced AKT phosphorylation, cancer cell invasion, angiogenesis, and the production of pro-inflammatory cytokines. It also reduced the expression of the cytokine granulocyte macrophage colony-stimulating factor and Snail in a dosage-dependent manner. Interestingly,using R428 to inhibit Axl-mediated cellular and molecular functions during cisplatin treatments achieved an enhanced suppression of liver metastases. Axl knockdowns in RAC cell lines reduced migration, invasion, and in vivo engraftment, accompanied by a downregulation in the activity of the Ral GTPase proteins (RalA and RalB). Similar effects were obtained using an A428 inhibitor. Blocking Axl functions also abrogated the phosphorylation of ERBB2 (Her-2/neu) at the Tyr877 residue, which reveals the cross-functional effects of R428 on different receptor signaling axes.
Cabozantinib (XL184) and R428 (BGB324) Inhibit the Growth of Esophageal Squamous Cell Carcinoma (ESCC)

Uses

R 428 is an AXL tyrosine kinase inhibitor shown to be used as an anti-cancer agent.

target

Axl

References

1) Holland?et al.?(2010),?R428, a Selective Small Molecule Inhibitor of Axl Kinase, Blocks Tumor Spread and Prolongs Survival in Models of Metastatic Breast Cancer;?Cancer Res.?70?1544 2) Fleuren?et al.?(2014),?The role of AXL and the in vitro activity of the receptor tyrosine kinase inhibitor BGB324 in Ewing sarcoma;?Oncotarget?5?12753 3) Xu?et al.?(2014),?Inhibition of Axl improves the targeted therapy against ALK-mutated neuroblastoma;?Biochem. Biophys. Res. Commun.?454?566 4) Ben-Batalla?et al.?(2017),?Axl Blockade by BGB324 Inhibits BCR-ABL Tyrosine Kinase Inhibitor-Sensitive and -Resistant Chronic Myeloid Leukemia;?Clin. Cancer Res.?23?2289 5) Lin?et al.?(2017),?Targeting AXL overcomes resistance to docetaxel therapy in advanced prostate cancer;?Oncotarget?8?41064 6) Guo?et al.?(2017),?Axl inhibition induces the antitumor immune response which can be further potentiated by PD-1 blockade in the mouse cancer models;?Oncotarget?8?89761 7) Ludwig?et al.?(2018),?Small-Molecule Inhibition of Axl Targets Tumor Immune

R428 Preparation Products And Raw materials

Raw materials

Preparation Products

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R428 Suppliers

China 142 India 2 United Kingdom 1 United States 17 Global 162

Twochem Co.Ltd.

Tel: 021-58111628 15800915896
Fax: QQ 3285589261
Country: China
ProdList: 1988
Advantage: 58

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: 0519-85788828 13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3553
Advantage: 58

Wuhan Shanhai Zhihe Biotechnology Co., Ltd.

Tel: 17771424646
Email: shoubull@126.com
Country: China
ProdList: 965
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: QQ:65489617 15618227136
Fax: 21-5161 9052
Email: info@SuperLan-chem.com
Country: China
ProdList: 9445
Advantage: 58

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2923
Advantage: 55

Jinan Trio PharmaTech Co., Ltd.

Tel: +86 (531) 88811783
Fax: +86 (531) 55696010 QQ 1762738062
Email: sales@trio-pharmatech.com (International market)
Country: China
ProdList: 1856
Advantage: 62

Shanghai Feibo Chemical Technology Co., Ltd

Tel: 021-58955608,2250286 15921236618
Email: blinkzeng@gmail.com
Country: China
ProdList: 523
Advantage: 62

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4647
Advantage: 58

Shanghai Topbiochem Technology Co., Ltd

Tel: 021-58170097
Email: info@topbiochem.com
Country: China
ProdList: 9442
Advantage: 58

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1494
Advantage: 55

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View Lastest Price from R428 manufacturers

Hebei Mojin Biotechnology Co., Ltd

Product: R428 1037624-75-1
Price: US $0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 50000KG/month
Release date: 2023-09-26

Hebei Guanlang Biotechnology Co., Ltd.

Product: R428 1037624-75-1
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 500000kg
Release date: 2022-10-26

Career Henan Chemical Co

Product: R428; R428 (BGB324) 1037624-75-1
Price: US $0.01/KG
Min. Order: 1KG
Purity: 98%; 99%
Supply Ability: 1kg；10kg; 25kg
Release date: 2020-01-07

1037624-75-1, R428Related Search:

ZM 447439 Imatinib mesylate Adapalene Vorinostat Bemcentinib(racemic) Binimetinib ARRY-424704, ARRY-704 BKM120 (NVP-BKM120, Buparlisib) MLN0905 2-[[(1R)-1-[7-methyl-2-(4-morpholinyl)-4-oxo-4h-pyrido[1,2-a]pyrimidin-9-yl]ethyl]amino]benzoic acid NVP-BVU 972 Tozasertib Nutlin 3a 6-[2-tert-Butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline 6-Amino-N-[3-[4-(4-morpholinyl)pyrido[3',2':4,5]furo[3,2-d]pyrimidin-2-yl]phenyl]-3-pyridinecarboxamide BMS-794833

(S)-1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)-1H-1,2,4-triazole-3,5-diamine

BGB-324

BGB-324, CPDB1725

(S)-1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-(7-(pyrrolidin-1-yl)-6,7,8

R428

R428 (BGB324)

1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-1H-1,2,4-triazole-3,5-diamine

EOS-62006

Bemcentinib

BGB324 (R428)

R428, 98%, a potent and selective inhibitor of Axl

BGB324(R428,Bemcentinib)

1-(6,7-dihydro-5H-benzo[2,3]cyclohepta[2,4-d]pyridazin-3-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine

R428-(R) (R428-P1)

CS-1130

Bemcentinib(R428,BGB324)

R-428; R 428;BGB-324;BGB 324

BEMCENTINIB (R428)

1H-1,2,4-Triazole-3,5-diamine, 1-(6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[(7S)-6,7,8,9-tetrahydro-7-(1-pyrrolidinyl)-5H-benzocyclohepten-2-yl]-

R428 USP/EP/BP

Bemcentinib intermediate

Bemcentinib BGB-324 R428

(S)-1-(6,7-Dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-yl)-N3-[7-(1-pyrrolidinyl)-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl]-1H-1,2,4-triazole-3,5-diamine

Bemcentinib Crude

R-428 (BEMCENTINIB)

1037624-75-1

C30H34N8

C31H35N7

Inhibitors

APIs

API