(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.
For research use only. We do not sell to patients.
- CAS No.: 1037624-76-2
- Formula: C30H34N8
- Molecular Weight:506.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
117.2 nM
Compound: 2; BGB324
|
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
|
[PMID: 33733758] |
| BaF3 | IC50 |
98.8 nM
Compound: 1; BGB324
|
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
|
[PMID: 36358010] |
Chemical Information
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CAS No. 1037624-76-2
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Molecular Weight 506.66
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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)