R428 free base · Synonyms: Bemcentinib | BGB-324

Bemcentinib is an inhibitor of Axl.

For research use only. Not for human or veterinary use.

Target TAM Receptor

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

R428 structure

CAS No.: 1037624-75-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 385.00	BP-01834-250mg	In stock	Get quote
500 mg	USD 685.00	BP-01834-500mg	In stock	Get quote
1 g	USD 1,085.00	BP-01834-1g	In stock	Get quote
5 g	Inquire	BP-01834-5g	Inquire	Inquire

Need another size or custom synthesis? Request a quote.

Description

Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

Biological activity

In Vitro Bemcentinib (R428) (2 μM) significantly interferes with mechanisms of migration and invasion of Axlpos melanoma cells at levels comparable to Axl knockdown. Bemcentinib (R428) synergizes with CDDP to enhance suppression of liver micrometastasis. Bemcentinib (R428) (50 nM-1 μM) causes a concentration-dependent inhibition of preadipocyte differentiation into mature adipocytes, as evidenced by reduced lipid uptake. 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. 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.

Identifiers

SMILES: NC1=NC(NC2=CC3=C(CC[C@@H](CC3)N3CCCC3)C=C2)=NN1C1=NN=C2C(CCCC3=CC=CC=C23)=C1
InChIKey: KXMZDGSRSGHMMK-VWLOTQADSA-N

Specifications

MW (average): 506.6446
Formula: C₃₀H₃₄N₈
CAS No.: 1037624-75-1
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO, not in water

Documents

References

[1]. Holland SJ, Pan A, Franci C, 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;70(4):1544-1554.

[2]. 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.

[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.

Same research area

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