Bemcentinib (GMP)
Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 1037624-75-1
- Formula: C30H34N8
- Molecular Weight:506.64
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Axl |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
0.94 μM
Compound: 1; R428, BGB-324
|
Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against mouse 4T1 cells highly expressing AXL after 72 hrs by MTT assay
|
[PMID: 35279611] |
| 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 |
117.2 nM
Compound: 8; R428; BGB324
|
Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
Antiproliferative activity against mouse BaF3 stably expressing human TEL-AXL incubated for 72 hrs
|
[PMID: 33957388] |
| 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] |
| GES1 | IC50 |
>60 μM
Compound: 1; R428, BGB-324
|
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
|
[PMID: 35279611] |
| HeLa | IC50 |
<30 nM
Compound: 17; BGB324; R428
|
Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
Inhibition of recombinant AXL in human HeLa cells after 1 hr by ELISA
|
[PMID: 26555154] |
| MCF-10A | IC50 |
>60 μM
Compound: 1; R428, BGB-324
|
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
|
[PMID: 35279611] |
| MDA-MB-231 | IC50 |
2.84 μM
Compound: 1; R428, BGB-324
|
Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells highly expressing AXL after 72 hrs by MTT assay
|
[PMID: 35279611] |
Bemcentinib (R428) (2 μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown[1].
Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis[2].
Bemcentinib (R428) (50 nM-1 μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) makes mice keep on a high-fat diet resulted in significantly reduced weight gain and subcutaneous and gonadal fat mass[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1037624-75-1
-
Molecular Weight 506.64
-
Formula C30H34N8
-
SMILES
NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6
-
Synonyms
R428 (GMP); BGB324 (GMP)
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)
Bemcentinib (GMP) Related Classifications
HY-15150G Related Classifications
Powered by Bioz