DC Chemicals Limited
China
Product Name: Bortezomib (Velcade,MG-341,PS-341)
Price: $200.0/100mg $400.0/250mg $800.0/1g
Purity: 98.0%
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Bortezomib
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: Bortezomib
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

179324-69-7

179324-69-7 structure

179324-69-7 structure

Name: Bortezomib (PS-341)
Chemical Name: bortezomib
CAS Number: 179324-69-7
Molecular Formula: C₁₉H₂₅BN₄O₄
Molecular Weight: 384.237
Catalog: API Antineoplastic agents Other antineoplastic agents
Create Date: 2018-02-07 08:00:00
Modify Date: 2024-01-02 12:20:03
Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.

Name	bortezomib
Synonyms	[(1R)-3-methyl-1-({(2S)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid Radiciol boronic acid, [(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl)amino]propyl]amino]butyl]- Bortezomib dpba BortezMib N-[(1R)-1-(Dihydroxyboryl)-3-methylbutyl]-Nα-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide MFCD05260688 BortezoMib-D8 Boronic acid, ((1R)-3-methyl-1-(((2S)-1-oxo-3-phenyl-2-((pyrazinylcarbonyl)amino)propyl)amino)butyl)- N-[(1R)-1-(Dihydroxyboryl)-3-methylbutyl]-Nα-(2-pyrazinylcarbonyl)-L-phenylalaninamide Velcade N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-Nα-(pyrazin-2-ylcarbonyl)-L-phenylalaninamide Boronic acid, B-[(1R)-3-methyl-1-[[(2S)-1-oxo-3-phenyl-2-[(2-pyrazinylcarbonyl)amino]propyl]amino]butyl]- BortezoMib Base MG-341 PS-341 BortezoMib for res

Description	Bortezomib (PS-341) is a potent 20S proteasome inhibitor with a Ki of 0.6 nM.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome Research Areas >> Cancer
Target	Ki: 0.6 nM (20S proteasome)[1]
In Vitro	Bortezomib (PS-341) effects proteins that control cell cycle progression. Treatment of PC-3 cells with Bortezomib (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. The Bortezomib doses at which 50% of PC-3 cells are killed at 24 and 48 h are determined to be 100 and 20 nM, respectively[1]. Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome. Inhibition of the proteasome by Bortezomib results in activation of JNK, stabilization of p53, Bid, Bax, p21, p27, caveolin-1, and IκBα, resulting in inhibition of NF-κB[2]. The IC50 of Bortezomib is found to be 2.46 nM for 26S proteasome in the B16F10 cells[3].
In Vivo	Mice bearing PC-3 tumors are treated with Bortezomib (i.v., 0.3 or 1.0 mg/kg). Bortezomib (1.0 mg/kg) results in a significant decrease in tumor growth ~60%. Bortezomib (0.3 mg/kg) produces a 16% decrease in tumor volume but did not reach significance[1]. Bortezomib (0.2 mg/kg) significantly decreases the withdrawal threshold on days 11 and 15 and increases the number of withdrawal responses on days 11 and 15 compared with the vehicle group in the von Frey and acetone tests[4].
Cell Assay	The human PC-3 prostate tumor cells are treated with Bortezomib (0.1 nM, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 24-48 h in complete medium. Cytotoxicity is measured using a MTT assay[1].
Animal Admin	Mice[1] Male nude mice (18-20 g; n=51) are used. Bortezomib (0.3 or 1.0 mg/kg) is administered in vehicle i.v. using a dose volume of 100 μL per mouse or directly into the tumor in a 10 μL volume. Due to the comparatively high levels of Bortezomib in the prostate, after i.v. dosing of radiolabeled drug, it is decided to examine the effects of this novel compound in the prostate, PC-3, xenograft tumor model. Animals are treated when the tumors become palpable (>300 mm3). Male nude mice (18-20 g; n=51) are used. Bortezomib (0.3 or 1.0 mg/kg) is administered in vehicle i.v. using a dose volume of 100 μL per mouse or directly into the tumor in a 10 μL volume. Due to the comparatively high levels of Bortezomib in the prostate, after i.v. dosing of radiolabeled drug, it is decided to examine the effects of this novel compound in the prostate, PC-3, xenograft tumor model. Animals are treated when the tumors become palpable (>300 mm3). Rats[4] Male Sprague-Dawley rats weighing 200-250 g are used. Bortezomib (0.05, 0.1, or 0.2 mg/kg) or vehicle (5% DMSO solution) is administered intraperitoneally (i.p.) twice a week for 2 weeks (on days 1, 4, 8, and 11). The administration schedule and doses of Bortezomib are determined based on clinical treatment (1.3 mg/m2 of Bortezomib on days 1, 4, 8, and 11).
References	[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22. [2]. Boccadoro M, et al. Preclinical evaluation of the proteasome inhibitor bortezomib in cancer therapy. Cancer Cell Int. 2005 Jun 1;5(1):18. [3]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9. [4]. Yamamoto S, et al. Behavioral and pharmacological characteristics of bortezomib-induced peripheral neuropathy in rats. J Pharmacol Sci. 2015 Sep;129(1):43-50.

Density	1.2±0.1 g/cm3
Melting Point	122-124°C
Molecular Formula	C₁₉H₂₅BN₄O₄
Molecular Weight	384.237
Exact Mass	384.196899
PSA	124.44000
LogP	2.45
Index of Refraction	1.564
Storage condition	Hygroscopic, -20°C Freezer, Under Inert Atmosphere
Stability	Hygroscopic and Moisture Sensitive

Hazard Codes	Xi
Safety Phrases	S26-S36/37/39
RIDADR	3261
HS Code	2934999090

205393-22-2 structure

205393-22-2

~71%

179324-69-7 structure

179324-69-7

Literature: WO2009/36281 A2, ; Page/Page column 41; 42-44; 47-48 ;

1029701-48-1 structure

1029701-48-1

~%

179324-69-7 structure

179324-69-7

Literature: Journal of the American Chemical Society, , vol. 130, # 22 p. 6910 - 6911

98-97-5 structure

98-97-5

1029701-41-4 structure

1029701-41-4

~%

179324-69-7 structure

179324-69-7

Literature: Journal of the American Chemical Society, , vol. 130, # 22 p. 6910 - 6911

789472-91-9 structure

789472-91-9

~%

179324-69-7 structure

179324-69-7

Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 1018 - 1029

1161-13-3 structure

1161-13-3

~%

179324-69-7 structure

179324-69-7

Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 1018 - 1029

514820-48-5 structure

514820-48-5

~%

179324-69-7 structure

179324-69-7

Literature: US2013/85277 A1, ;

13734-34-4 structure

13734-34-4

~%

179324-69-7 structure

179324-69-7

Literature: WO2014/41324 A1, ;

Precursor 6
205393-22-2 98-97-5 1029701-41-4 789472-91-9
1161-13-3 13734-34-4
DownStream 1
114457-94-2

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%