Bemcentinib (Synonyms: R428; BGB324)

Name: Bemcentinib
Brand: MedChemExpress
SKU: HY-15150
Rating: 5.0 (62 reviews)

Cat. No.: HY-15150 Pureté: 99.92%: Fiche technique
COA

SDS
Instruction de manipulation
FAQs
Technical Support

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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No. : 1037624-75-1

Size	Stock	Quantité

Échantillon gratuit (0.1 - 0.2 mg)	Appliquer maintenant
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	En stock	Estimated Time of Arrival: December 31
500 mg	Obtenir un devis
1 g	Obtenir un devis

or Bulk Inquiry

* Veuillez sélectionner la quantité avant d'ajouter des articles.

This product is a controlled substance and not for sale in your territory.

Avis client

Based on 62 publication(s) in Google Scholar

Other Forms of Bemcentinib:

Bemcentinib (Standard) In-stock
Bemcentinib-d₈ Obtenir un devis
Bemcentinib (GMP) Obtenir un devis

62 Publications Citing Use of MCE Bemcentinib

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2023 Feb 22;10(1):7. [Abstract]; Bemcentinib (BGB324; 1 μM; 30 min) partially blocks the activation of HSC by rGAS6 in LX-2 cells.

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4. [Abstract]; Western blot showing phosphorylated PLCγ2 in cells treated with gef (1 μM) and R428 or Lapa for 24 hr. SE, short exposure; LE, long exposure.

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Dec 10;34(6):954-969.e4. [Abstract]; Western blot showing PKCδ expression in nuclear extracts of GR4 and GR10 cells treated with 1 μM gef in combination with 2.5 μM R428 and 5 μM GW572016 (Lapa) for 24 hr.

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]; BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of TAM receptor (LDC1267 at 1 µM, UNC2250 at 5 µM, R428 at 5 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Dec 19;7(1):17770. [Abstract]; Western blot analysis of pAXL level in H1299 cells treated with the indicated concentration of R428 for 1 h. Results are confirmed in three independent experiments.

: Bemcentinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 20;8(25):41064-41077. [Abstract]; The expression of AXL in the PC3-DR and DU145-DR cells treated with R428 (1 μM) is analyzed by western blotting.

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform TAM Receptor:

Voir toutes les isoformes

Axl Mer Tyro3

Activité biologique
Protocole
Pureté et documentation
Références
Avis client

Description

IC₅₀ & Target

Axl

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.94 3 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]
4T1	IC₅₀	0.94 3 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]
4T1	IC₅₀	0.94 3 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 1 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	117.2 1 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]
GES1	IC₅₀	>60 3 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]
BaF3	IC₅₀	117.2 1 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]
MCF-10A	IC₅₀	>60 3 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]
GES1	IC₅₀	> 60 3 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]
BaF3	IC₅₀	98.8 1 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]
MDA-MB-231	IC₅₀	2.84 3 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]
HeLa	IC₅₀	< 30 1 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]
BaF3	IC₅₀	117.2 1 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]
MCF-10A	IC₅₀	> 60 3 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]
HeLa	IC₅₀	<30 1 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]
MDA-MB-231	IC₅₀	2.84 3 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]
GES1	IC₅₀	> 60 3 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 1 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 3 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 3 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.

Essai clinique

Masse moléculaire

506.64

Formule

C₃₀H₃₄N₈

CAS No.

1037624-75-1

Appearance

Solid

Color

Off-white to yellow

SMILES

NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (24.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9738 mL	9.8689 mL	19.7379 mL
5 mM	0.3948 mL	1.9738 mL	3.9476 mL
10 mM	0.1974 mL	0.9869 mL	1.9738 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité
Calculateur de dilution

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.47 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.92%

Select Batch:

Fiche technique (285 KB) SDS (396 KB)

COA (260 KB) HNMR (300 KB) RP-HPLC (242 KB) LCMS (99 KB) Elemental Analysis Report (117 KB)

Instruction de manipulation (2659 KB)

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]

Test cellulaire ^[1]	Cells maintained for 24 hours in serum-free medium are harvested and transferred to the upper chamber (1.5×10⁵ cells per well) of uncoated (migration) or matrigel-coated (invasion) 24-well chambers. RPMI medium containing 10% fetal bovine serum is added to the lower chamber. Bemcentinib (R428) (2 μM) or vehicle (DMSO, 0.25%) is added for 2 hours to cells before loading them in the upper chambers. Both the upper and lower chambers contain the drug or vehicle. Quantification of migrating/invading cells is obtained by measuring their fluorescent signals with a 480/520 nm filter set on an Infinite M1000 microplate reader 20 or 42 hours later, respectively. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[2]	Seven- to 8-wk-old female NCr nu/nu mice are injected intracardially with bioluminescent MDA-MB-231-luc-D3H2LN cell suspension. Oral dosing with Bemcentinib (R428) (125 mg/kg, p.o.) or vehicle twice daily begins 2 h before cell implantation and continue to day 21 (n=20). Metastatic burden is quantified by in vivo bioluminescence imaging on day 22 and analyzed using the Wilcoxon rank sum test. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9738 mL	9.8689 mL	19.7379 mL	49.3447 mL
	5 mM	0.3948 mL	1.9738 mL	3.9476 mL	9.8689 mL
	10 mM	0.1974 mL	0.9869 mL	1.9738 mL	4.9345 mL
	15 mM	0.1316 mL	0.6579 mL	1.3159 mL	3.2896 mL
	20 mM	0.0987 mL	0.4934 mL	0.9869 mL	2.4672 mL

Bemcentinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bemcentinib1037624-75-1R428 BGB324R 428R-428BGB324BGB 324BGB-324TAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Nom du produit			Requested Quantity *
Nom du demandeur *			Civilité
Adresse e-mail *			Numéro de téléphone *
Department			Nom de l'organisation *
City			État
Country or Region *
Remarques

Nom du produit			Lot #
Nom du demandeur *			Adresse e-mail *
Numéro de téléphone			Department *
Nom de l'organisation *			Country or Region *
Remarques

Nom
Email *

	Sorry, but the email address you supplied was invalid.

Bemcentinib (Synonyms: R428; BGB324)

Avis client

Other Forms of Bemcentinib:

Bemcentinib Related Antibodies

62 Publications Citing Use of MCE Bemcentinib

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform TAM Receptor:

Activité biologique

Protocole

Pureté et documentation

Références

Avis client

Bemcentinib Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Bemcentinib Related Classifications

Keywords:

Vos produits récemment consultés:

Avis client

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report