Bemcentinib
Based on 63 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 1037624-75-1
- 分子式: C30H34N8
- 分子量:506.64
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Bemcentinib
More- Signal Transduct Target Ther. 2026 Jun 17;11(1):238. [Abstract]
- Science. 2025 Feb 21;387(6736):892-900. [Abstract]
- Cancer Cell. 2025 Feb 10;43(2):269-291.e19. [Abstract]
- Cancer Cell. 2024 Oct 14;42(10):1693-1712.e24. [Abstract]
- Cancer Cell. 2018 Dec 10;34(6):954-969.e4. [Abstract]
- Cell. 2026 May 28;189(11):3444-3464.e28. [Abstract]
- Mil Med Res. 2023 Feb 22;10(1):7. [Abstract]
- Eur Respir J. 2025 Jan 9:2400615. [Abstract]
- Cell Stem Cell. 2020 Jul 2;27(1):125-136.e7. [Abstract]
- Cancer Res. 2026 Mar 5. [Abstract]
- Nat Commun. 2023 Jun 15;14(1):3560. [Abstract]
- Neuron. 2022 Nov 16;110(22):3711-3726.e16. [Abstract]
- Theranostics. 2018 Jul 30;8(15):4262-4278. [Abstract]
- Cell Rep Med. 2025 Dec 29:102526. [Abstract]
- Cell Commun Signal. 2024 Dec 18;22(1):598. [Abstract]
- J Pharm Anal. 2025 May;15(5):101092. [Abstract]
- Acta Pharmacol Sin. 2023 May;44(5):984-998. [Abstract]
- Cell Syst. 2020 Nov 18;11(5):478-494.e9. [Abstract]
- Biomed Pharmacother. 2021 Dec:144:112347. [Abstract]
- Cell Rep. 2021 Apr 6;35(1):108959. [Abstract]
- Br J Cancer. 2025 Nov 26. [Abstract]
- Cell Mol Life Sci. 2022 May 27;79(6):316. [Abstract]
- EMBO Rep. 2020 Nov 5;21(11):e50078. [Abstract]
- JCI Insight. 2020 Oct 15;5(20):e141321. [Abstract]
- Protein Sci. 2024 Apr;33(4):e4948. [Abstract]
- Commun Biol. (2021) 4:1002.
- Commun Biol. 2021 Aug 24;4(1):1002. [Abstract]
- Transplantation. 2022 Jul 1;106(7):1351-1364. [Abstract]
- Pharmaceuticals (Basel). 2023 May 6;16(5):703. [Abstract]
- Cell Rep Methods. 2023 Dec 18;3(12):100663. [Abstract]
- FEBS J. 2025 Oct 28. [Abstract]
- J Mol Med (Berl). 2025 Sep;103(9):1043-1053. [Abstract]
- J Cell Mol Med. 2025 Jan;29(1):e70321. [Abstract]
- FEBS J. 2025 Jan;292(1):115-128. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2022 Dec 1;1868(12):166490. [Abstract]
- J Cell Mol Med. 2019 Aug;23(8):5518-5531. [Abstract]
- Am J Physiol Heart Circ Physiol. 2022 Nov 1;323(5):H917-H933. [Abstract]
- Antiviral Res. 2025 Dec:244:106307. [Abstract]
- Sci Rep. 2017 Dec 19;7(1):17770. [Abstract]
- J Virol. 2025 Aug 25:e0022125. [Abstract]
- BMC Cancer. 2021 Jun 17;21(1):713. [Abstract]
- Int J Biochem Cell Biol. 2025 Feb 1:180:106750. [Abstract]
- Genes (Basel). 2022 Nov 2;13(11):2011. [Abstract]
- Genes (Basel). 2020 Dec 23;12(1):9. [Abstract]
- World J Surg Oncol. 2022 Oct 6;20(1):334. [Abstract]
- Exp Ther Med. 2020 Nov;20(5):41. [Abstract]
- Head Neck. 2023 May;45(5):1255-1271. [Abstract]
- Technical University of Dresden. 2025.
- J Mazandaran Univ Med Sci. 2025; 35 (251):15-29.
- bioRxiv. 2025 Aug 13.
- bioRxiv. 2025 May 30.
- bioRxiv. 2025 May 21.
- bioRxiv. 2024 Aug 6:2024.08.05.606734. [Abstract]
- Preprints. 2023 Sep 28.
- Research Square Preprint. 2023 Jul 3.
- bioRxiv. 2023 Jun 11.
- Nencki Institute of Experimental Biology. 2022 Oct.
- Research Square Preprint. 2021 Dec.
- bioRxiv. 2020 Jun.
- bioRxiv. 2020 Apr.
- bioRxiv. 2020 Mar.
- University of Oslo. 2019 Feb.
- Oncotarget. 2017 Jun 20;8(25):41064-41077. [Abstract]
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生物活性
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Axl |
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Cell Line
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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: 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 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
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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
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[PMID: 36358010] |
| GES1 | IC50 |
>60 μM
Compound: 1; R428, BGB-324
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Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
Cytotoxicity against human GES1 cells after 72 hrs by MTT assay
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[PMID: 35279611] |
| HeLa | IC50 |
<30 nM
Compound: 17; BGB324; R428
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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
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[PMID: 26555154] |
| MCF-10A | IC50 |
>60 μM
Compound: 1; R428, BGB-324
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Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells after 72 hrs by MTT assay
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[PMID: 35279611] |
| MDA-MB-231 | IC50 |
2.84 μM
Compound: 1; R428, BGB-324
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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
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[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1037624-75-1
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性状 Solid
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分子量 506.64
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分子式 C30H34N8
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Color Off-white to yellow
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SMILES
NC1=NC(NC2=CC(CC[C@@H](N3CCCC3)CC4)=C4C=C2)=NN1C(N=N5)=CC6=C5C7=CC=CC=C7CCC6
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別名
R428; BGB324
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (63)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Targeting oncogenic TβRI signaling inhibits androgen-independent prostate cancer growth and metastasis. [Abstract]2026 Jun 17;11(1):238. PMID: 42303991 -
Science
2025 Feb 21;387(6736):892-900. PMID: 39977508 -
Cancer Cell
Adiponectin reduces immune checkpoint inhibitor-induced inflammation without blocking anti-tumor immunity. [Abstract]2025 Feb 10;43(2):269-291.e19. PMID: 39933899 -
Cancer Cell
Distinct tumor architectures and microenvironments for the initiation of breast cancer metastasis in the brain. [Abstract]2024 Oct 14;42(10):1693-1712.e24. PMID: 39270646 -
Cancer Cell
Targeting PKCδ as a Therapeutic Strategy against Heterogeneous Mechanisms of EGFR Inhibitor Resistance in EGFR-Mutant Lung Cancer. [Abstract]2018 Dec 10;34(6):954-969.e4. PMID: 30537515
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.
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Cell
2026 May 28;189(11):3444-3464.e28. PMID: 41923641 -
Mil Med Res
Single-cell transcriptomic dissection of the cellular and molecular events underlying the triclosan-induced liver fibrosis in mice. [Abstract]2023 Feb 22;10(1):7. PMID: 36814339
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.
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Eur Respir J
Inhibition of AXL ameliorates pulmonary fibrosis via attenuation of M2 macrophage polarization. [Abstract]2025 Jan 9:2400615. PMID: 39788632 -
Cell Stem Cell
A Human Pluripotent Stem Cell-based Platform to Study SARS-CoV-2 Tropism and Model Virus Infection in Human Cells and Organoids. [Abstract]2020 Jul 2;27(1):125-136.e7. PMID: 32579880 -
Cancer Res
Metronomic Chemotherapy Induces Metabolic Reprogramming in Cancer Cells That Modulates Mature Regulatory Dendritic Cell Function to Stimulate Antitumor Immunity. [Abstract]2026 Mar 5. PMID: 41784618 -
Nat Commun
CNK2 promotes cancer cell motility by mediating ARF6 activation downstream of AXL signalling. [Abstract]2023 Jun 15;14(1):3560. PMID: 37322019 -
Neuron
Uncompetitive, adduct-forming SARM1 inhibitors are neuroprotective in preclinical models of nerve injury and disease. [Abstract]2022 Nov 16;110(22):3711-3726.e16. PMID: 36087583 -
Theranostics
Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]2018 Jul 30;8(15):4262-4278. PMID: 30128052
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.
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Cell Rep Med
CDK4/6 inhibition overcomes venetoclax resistance mechanisms with enhanced combination activity in acute myeloid leukemia. [Abstract]2025 Dec 29:102526. PMID: 41468895 -
Cell Commun Signal
CD91-mediated reprogramming of DCs by immunogenic heat shock proteins requires the kinases AXL and Fgr. [Abstract]2024 Dec 18;22(1):598. PMID: 39696592 -
J Pharm Anal
Screen of FDA-approved drug library identifies vitamin K as anti-ferroptotic drug for osteoarthritis therapy through Gas6. [Abstract]2025 May;15(5):101092. PMID: 40496065 -
Acta Pharmacol Sin
Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. [Abstract]2023 May;44(5):984-998. PMID: 36450791 -
Cell Syst
Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]2020 Nov 18;11(5):478-494.e9. PMID: 33113355 -
Biomed Pharmacother
Overcoming PLK1 inhibitor resistance by targeting mevalonate pathway to impair AXL-TWIST axis in colorectal cancer. [Abstract]2021 Dec:144:112347. PMID: 34700228 -
Cell Rep
Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2. [Abstract]2021 Apr 6;35(1):108959. PMID: 33811811 -
Br J Cancer
Crosstalk of NPY and TGFβ orchestrates the signaling to facilitate perineural invasion of oral squamous cell carcinoma. [Abstract]2025 Nov 26. PMID: 41298817 -
Cell Mol Life Sci
2022 May 27;79(6):316. PMID: 35622156 -
EMBO Rep
The actin modulator hMENA regulates GAS6-AXL axis and pro-tumor cancer/stromal cell cooperation. [Abstract]2020 Nov 5;21(11):e50078. PMID: 32909687 -
JCI Insight
Single cell transcriptomics of mouse kidney transplants reveals a myeloid cell pathway for transplant rejection. [Abstract]2020 Oct 15;5(20):e141321. PMID: 32970632 -
Protein Sci
Identification of a novel DNA repair inhibitor using an in silico driven approach shows effective combinatorial activity with genotoxic agents against multidrug-resistant Escherichia coli. [Abstract]2024 Apr;33(4):e4948. PMID: 38501485 -
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Commun Biol
2021 Aug 24;4(1):1002. PMID: 34429509 -
Transplantation
Activated AXL Protects Against Hepatic Ischemia-reperfusion Injury by Upregulating SOCS-1 Expression. [Abstract]2022 Jul 1;106(7):1351-1364. PMID: 35546091 -
Pharmaceuticals (Basel)
Gas6/Axl Axis Activation Dampens the Inflammatory Response in Osteoarthritic Fibroblast-like Synoviocytes and Synovial Explants. [Abstract]2023 May 6;16(5):703. PMID: 37242486 -
Cell Rep Methods
AA2P-mediated DNA demethylation synergizes with stem cell agonists to promote expansion of hematopoietic stem cells. [Abstract]2023 Dec 18;3(12):100663. PMID: 38070507 -
FEBS J
Single-cell RNA sequencing reveals the protective role of renal Cx3cr1+ macrophages in cisplatin-induced acute kidney injury. [Abstract]2025 Oct 28. PMID: 41147753 -
J Mol Med (Berl)
Sex hormone-binding globulin restrains hepatic fibrosis via inhibition of Tgfβ expression. [Abstract]2025 Sep;103(9):1043-1053. PMID: 40616670 -
J Cell Mol Med
Orderly Regulation of Macrophages and Fibroblasts by Axl in Bleomycin-Induced Pulmonary Fibrosis in Mice. [Abstract]2025 Jan;29(1):e70321. PMID: 39779468 -
FEBS J
The AXL inhibitor bemcentinib overcomes microenvironment-mediated resistance to pioglitazone in acute myeloid leukemia. [Abstract]2025 Jan;292(1):115-128. PMID: 39325663 -
Biochim Biophys Acta Mol Basis Dis
AXL and MERTK receptor tyrosine kinases inhibition protects against pancreatic necrosis via selectively limiting CXCL2-related neutrophil infiltration. [Abstract]2022 Dec 1;1868(12):166490. PMID: 35841983 -
J Cell Mol Med
Long non-coding RNA LINC00526 represses glioma progression via forming a double negative feedback loop with AXL. [Abstract]2019 Aug;23(8):5518-5531. PMID: 31240814 -
Am J Physiol Heart Circ Physiol
Role of Axl in target organ inflammation and damage due to hypertensive aortic remodeling. [Abstract]2022 Nov 1;323(5):H917-H933. PMID: 36083796 -
Antiviral Res
Repurposed doxepin targeting host AXL kinase to disrupt viral 2C-mediated immune evasion in Coxsackievirus B infection. [Abstract]2025 Dec:244:106307. PMID: 41197812 -
Sci Rep
Cell softening in malignant progression of human lung cancer cells by activation of receptor tyrosine kinase AXL. [Abstract]2017 Dec 19;7(1):17770. PMID: 29259259
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.
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J Virol
SFTSV utilizes AXL/GAS6 for entry via PI3K-PLC-dependent macropinocytosis activated by AXL-kinase. [Abstract]2025 Aug 25:e0022125. PMID: 40853130 -
BMC Cancer
AXL receptor tyrosine kinase: a possible therapeutic target in acute promyelocytic leukemia. [Abstract]2021 Jun 17;21(1):713. PMID: 34140003 -
Int J Biochem Cell Biol
2025 Feb 1:180:106750. PMID: 39900236 -
Genes (Basel)
Integrative Transcriptomic Analysis Identify Potential m6A Pathway-Related Drugs That Inhibit Cancer Cell Proliferation. [Abstract]2022 Nov 2;13(11):2011. PMID: 36360248 -
Genes (Basel)
2020 Dec 23;12(1):9. PMID: 33374832 -
World J Surg Oncol
AXL, along with PROS1, is overexpressed in papillary thyroid carcinoma and regulates its biological behaviour. [Abstract]2022 Oct 6;20(1):334. PMID: 36203174 -
Exp Ther Med
Pharmaceutical inhibition of AXL suppresses tumor growth and invasion of esophageal squamous cell carcinoma. [Abstract]2020 Nov;20(5):41. PMID: 32952632 -
Head Neck
Dual Axl/MerTK inhibitor INCB081776 creates a proinflammatory tumor immune microenvironment and enhances anti-PDL1 efficacy in head and neck cancer. [Abstract]2023 May;45(5):1255-1271. PMID: 36939040 -
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bioRxiv
Human Vascularized Macrophage-Islet Organoids to Model Immune-Mediated Pancreatic β cell Pyroptosis upon Viral Infection. [Abstract]2024 Aug 6:2024.08.05.606734. PMID: 39149298 -
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Oncotarget
2017 Jun 20;8(25):41064-41077. PMID: 28455956
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.
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
-
+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[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
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.
| 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 |