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Cat. No.: HY-15150G

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Bemcentinib (GMP)

(Synonyms: R428 (GMP); BGB324 (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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 1037624-75-1
화학식: C₃₀H₃₄N₈
분자량:506.64

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (280 KB)

Bemcentinib (GMP) Chemical Structure

CAS No.: 1037624-75-1

사이즈

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

Axl

All TAM Receptor Isoforms :

Cellular Effect

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]

In Vitro

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.

In Vivo

Bemcentinib (R428) (125 mg/kg, p.o.) significantly blocks MDA-MB-231-luc-D3H2LN metastases development in two independent mouse models of breast cancer dissemination, suppresses both tumor angiogenesis and vascular endothelial growth factor (VEGF)-induced corneal neovascularization in vivo^[2].
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
분자량 506.64
화학식 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)
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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Bemcentinib (GMP)

All TAM Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

Bemcentinib (GMP) Related Classifications

HY-15150G Related Classifications