Sorafenib (Synonyms: BAY 43-9006)

Name: Sorafenib
Brand: GlpBio
SKU: GC17369
Availability: InStock
Rating: 5 (30 reviews)

カタログ番号GC17369

ソラフェニブは、Raf-1とB-Rafをターゲットとするマルチキナーゼ阻害剤であり、それぞれのIC₅₀値は6 nMおよび22 nMです。

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Sorafenib 化学構造

Cas No.: 284461-73-0

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10mM (in 1mL DMSO)	$35.00	在庫あり
10mg	$32.00	在庫あり
50mg	$46.00	在庫あり
100mg	$60.00	在庫あり
500mg	$84.00	在庫あり

Tel：(909) 407-4943 Email: sales@glpbio.com

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カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 5 publications

Description Protocol Chemical Properties Product Documents

Product Documents

Quality Control & SDS

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Purity: >99.50%

Protocol

*In vitro* Kinase Assays with Recombinant Raf-1, BRAF, V599E BRAF, MEK-1, and ERK1^[1]:
Preparation method	Test compound inhibition against various RAF kinase isoforms, sorafenib was added to a mixture of Raf-1 (80 ng), wt BRAF, or V599E BRAF (80 ng) with MEK-1 (1 μg) in assay buffer [20 mmol/L Tris (pH 8.2), 100 mmol/L NaCl, 5 mmol/L MgCl₂, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The RAF kinase assay (final volume of 50 μL) was initiated by adding 25 μL of 10 μmol/L γ-^[33P]ATP (400 Ci/mol) and incubated at 32℃ for 25 minutes. Phosphorylated MEK-1 was harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid was used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter was used to quantify filter-bound radioactivity.
Applications	Sorafenib inhibited Raf-1 with IC₅₀ of 6nM; Sorafenib inhibited B-Raf activity of wild type and V599E mutant with IC₅₀ of 22 nM and 38 nM, respectively; Sorafenib has no activity against ERK-1, MEK-1.
Cell experiment ^[2]:
Cell lines	HSC-T6 cells
Preparation method	Cells were seeded into 96-well plates. When the cell density reached 70%, different concentrations of sorafenib were added, and equal amounts of DMSO without drug were exposed to the control group for 24 h.
Reaction Conditions	5-40μM; 24 h
Applications	HSC-T6 cell viability was dose-dependently inhibited by sorafenib at concentrations ranging from 5 to 40 μM.
Animal experiment ^[2]:
Animal models	Male C57BL/6 mice (6-8 weeks)
Preparation method	Mice were randomly divided into five groups (n=6 per group) including the vehicle group, CCl₄-treated group, CCl₄+sorafenib (2.5, 5, 10 mg/kg)-treated groups. The groups treated with CCl₄, CCl₄ + sorafenib were subjected intraperitoneal injections of olive oil with 10% CCl₄ for 8 weeks to induce liver fibrosis. The vehicle group was subjected intraperitoneal injections of the same dose of olive oil. After 4 weeks, each mouse in the groups treated with CCl₄ + sorafenib was orally administered sorafenib daily. The vehicle group and the CCl₄-treated group were orally administered the same dose of saline daily.
Dosage form	2.5, 5, 10 mg/kg; i.p; twice a week for 8 weeks
Applications	Sorafenib attenuated liver injury and ECM accumulation in CCl₄ -induced fibrotic livers.
References: [1]. Wilhelm SM, Carter C, et,al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. doi: 10.1158/0008-5472.CAN-04-1443. PMID: 15466206. [2]. Yuan S, Wei C, et,al.Sorafenib attenuates liver fibrosis by triggering hepatic stellate cell ferroptosis via HIF-1α/SLC7A11 pathway. Cell Prolif. 2022 Jan;55(1):e13158. doi: 10.1111/cpr.13158. Epub 2021 Nov 22. PMID: 34811833; PMCID: PMC8780895.

Sorafenib acts as a multi-kinase inhibitor, targeting Raf-1 and B-Raf with IC₅₀ values of 6 nM and 22 nM, respectively. Additionally, Sorafenib demonstrates inhibitory effects on VEGFR-2, VEGFR-3, PDGFR-β, Flt-3, and c-KIT, displaying corresponding IC₅₀ values of 90 nM, 20 nM, 57 nM, 59 nM, and 68 nM. Beyond these kinase activities, Sorafenib is capable of inducing autophagy and apoptosis while triggering ferroptosis activation, resulting in its notable antitumor efficacy ^[1-3].

Sorafenib(5-40μM; 24 h) had a dose-dependent inhibitory effect on HSC-T6 cells viability ^[4]. Sorafenib(25mM;0-42h) alters the lipid composition in Huh7.5 cells^[5].

Sorafenib(2.5, 5, 10 mg/kg; i.p; twice a week for 8 weeks) attenuated liver injury and extracellular matrix (ECM) accumulation in CCl₄ -induced fibrotic livers, accompanied by reduction of SLC7A11 and GPX4 proteins^[4]. Treatment with erastin and sorafenib(10 mg/kg; i.p; once every other day) alleviated liver fibrosis in mice by inducing hepatic stellate cells(HSCs) ferroptosis in mice^[6].The synergism of sorafenib and T cells is mediated via reduced ATF4 expression, causing activation of the IRF7-IL-15 axis in leukemia cells and thereby leading to metabolic reprogramming of leukemia-reactive T cells in humans^[7].

References:

[1]. Abdelgalil AA, Alkahtani HM, et,al.Sorafenib. Profiles Drug Subst Excip Relat Methodol. 2019;44:239-266. doi: 10.1016/bs.podrm.2018.11.003. Epub 2019 Jan 18. PMID: 31029219.

[2]. Wilhelm SM, Carter C, et,al.BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. doi: 10.1158/0008-5472.CAN-04-1443. PMID: 15466206.

[3]. Xia S, Pan Y, et,al.The microenvironmental and metabolic aspects of sorafenib resistance in hepatocellular carcinoma. EBioMedicine. 2020 Jan;51:102610. doi: 10.1016/j.ebiom.2019.102610. Epub 2020 Jan 6. PMID: 31918403; PMCID: PMC7000339.

[4]. Yuan S, Wei C, et,al. Sorafenib attenuates liver fibrosis by triggering hepatic stellate cell ferroptosis via HIF-1α/SLC7A11 pathway. Cell Prolif. 2022 Jan;55(1):e13158. doi: 10.1111/cpr.13158. Epub 2021 Nov 22. PMID: 34811833; PMCID: PMC8780895.

[5]. Liu G, Kuang S, et,al.Sorafenib kills liver cancer cells by disrupting SCD1-mediated synthesis of monounsaturated fatty acids via the ATP-AMPK-mTOR-SREBP1 signaling pathway. FASEB J. 2019 Sep;33(9):10089-10103. doi: 10.1096/fj.201802619RR. Epub 2019 Jun 14. PMID: 31199678.

[6]. Zhang Z, Guo M, et,al. RNA-binding protein ZFP36/TTP protects against ferroptosis by regulating autophagy signaling pathway in hepatic stellate cells. Autophagy. 2020 Aug;16(8):1482-1505. doi: 10.1080/15548627.2019.1687985. Epub 2019 Nov 11. PMID: 31679460; PMCID: PMC7469536.

[7]. Mathew NR, Baumgartner F,et,al. Sorafenib promotes graft-versus-leukemia activity in mice and humans through IL-15 production in FLT3-ITD-mutant leukemia cells. Nat Med. 2018 Mar;24(3):282-291. doi: 10.1038/nm.4484. Epub 2018 Feb 12. Erratum in: Nat Med. 2018 Apr 10;24(4):526. PMID: 29431743; PMCID: PMC6029618.

Cas No.	284461-73-0	SDF
同義語	BAY 43-9006
Chemical Name	4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide
Canonical SMILES	CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
Formula	C₂₁H₁₆ClF₃N₄O₃	M.Wt	464.82
溶解度	≥ 23.25mg/mL in DMSO	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.1514 mL	10.7569 mL	21.5137 mL
	5 mM	0.4303 mL	2.1514 mL	4.3027 mL
	10 mM	0.2151 mL	1.0757 mL	2.1514 mL

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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Sorafenib (Synonyms: BAY 43-9006)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 5 publications

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

レビュー

Sorafenib (Synonyms: BAY 43-9006)

顧客レビュー

GlpBio Citations

Bioactive Compounds Premium Provider

Product has been cited by 5 publications

Product Documents

Quality Control & SDS

Protocol

Complete Stock Solution Preparation Table

モルアリティ計算機

希釈計算機

In vivo Formulation Calculator (Clear solution)

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