(R)-Bemcentinib
(R)-Bemcentinib ((R)-R428) is the R-isomer of Bemcentinib (HY-15150). Bemcentinib (R428) is a selective, orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib blocks tumor metastasis and prolongs survival in metastatic breast cancer models.
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- CAS No.: 1037624-76-2
- Formule: C30H34N8
- Masse moléculaire:506.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
117.2 nM
Compound: 2; BGB324
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Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
Antiproliferative activity against mouse BaF3/TEL-AXL cells incubated for 72 hrs by SRB or CCK8 assay
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[PMID: 33733758] |
| BaF3 | IC50 |
98.8 nM
Compound: 1; BGB324
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Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs
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[PMID: 36358010] |
Chemical Information
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CAS No. 1037624-76-2
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Masse moléculaire 506.66
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Formule C30H34N8
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SMILES
NC=1N(C=2C=C3C(C=4C(CCC3)=CC=CC4)=NN2)N=C(NC=5C=C6C(=CC5)CC[C@H](CC6)N7CCCC7)N1
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Synonyms
(R)-R428; (R)-BGB324
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131(12):2448-57. [Content Brief]
[2]. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54. [Content Brief]
[3]. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(R)-Bemcentinib Related Classifications
HY-15150C Related Classifications
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