Bortezomib CAS: 179324-69-7
MF: C19H25BN4O4
MW: 384.24

Bortezomib (CAS 179324-69-7)

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Bortezomib is rated 5.0 out of 5 by 2.
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Nombres Alternativos: Bortezomib also known as Velcade; Radiciol; LDP-341
Solicitud: Bortezomib is a selective and robust 26S proteasome inhibitor and is a boronic acid dipeptide derivative
Número de CAS: 179324-69-7
Pureza: ≥98%
Peso Molecular: 384.24
Fórmula Molecular: C19H25BN4O4
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
* En el Certificado de Análisis específico de lote, puede encontrar información específica (como el contenido en agua).

Bortezomib is a selective and robust 26S proteasome inhibitor, that is a boronic acid dipeptide derivative. Human pancreatic cancer cell studies demonstrate Bortezomib to inhibit the PKR-like endoplasmic reticulum (ER) kinase and enhance ER stress, leading to apoptosis. Studies suggest that Bortezomib affects the gene expression of WT1, and blocks the function of human plasmacytoid DCs through the inhibition of intracellular trafficking of Toll-like receptors and modification of the ER homeostasis. Additionally, Bortezomib has been reported to inhibit necrosis and cell proliferation, and downregulate metastatic gene expression. Bortezomib is an inhibitor of 20S Proteasome.


References

1. Lightcap, E.S. et al. 2000. Clin. Chem. 46(5): 673-683. PMID: 10794750

2. Adams, J. 2002. Oncologist. 7(1): 9-16. PMID: 11854543

3. Ling, Y.H. et al. 2003. Clin. Cancer Res. 9(3): 1145-1154. PMID: 12631620

5. Nawrocki, S.T., et al. 2005. Cancer Res. 65: 11510-11519. PMID: 16357160

6. Hirai, M., et al. 2010. Blood. [Epub ahead of print]. PMID: 20956804

7. Jones, M.D., et al. 2010. Clin. Cancer Res. 16: 4978-4989. PMID: 20843837

8. Alimena, G., et al. 2010. Leuk Res. [Epub ahead of print]. PMID: 20971509

9. Dou, Q.P. and Zonder, J.A. 2014. Curr Cancer Drug Targets. 14(6): 517-536. PMID: 25092212

Uso :
A stock solution can be made by dissolving in DMSO, DMF and purge with inert gas. 20 mg/ml.
Estado de Materia :
Solid
Solubilidad :
Soluble in chloroform, DMSO (200 mg/ml), ethanol (200 mg/ml), and methanol. Partly miscible in water.Maximum solubility in plain water is estimated to be about 5-10 µM. Buffers, serum, or other additives may increase or decrease the aqueous solubility.
ALMACENAMIENTO :
Store at -20° C
Punto de Fusión :
139-143° C
Punto de ebullición :
684.30° C (Predicted)
Densidad :
1.21 g/cm3 (Predicted)
Indice de Refracción :
n20D 1.56 (Predicted)
IC50 :
20S proteasome: IC50 = 0.16 nM (mouse); A2780: IC50 = 1.7 nM (human); U266: IC50 = 2.45 nM (human); RPMI18226: IC50 = 3.5 nM (human); HL-60: IC50 = 3.5 nM (human)
Datos Ki :
20S proteasome: Ki= 0.55 nM; Beta-chymotrypsin: Ki= 320 nM (human); Cathepsin G: Ki= 630 nM (human); 26S proteasome: Ki= 6 nM
Valores de pK :
pKa: 13.82 (Predicted)
Para Uso Exclusivo en Investigación. No está diseñado para uso en diagnosis o terapia.
RTECS :
ED7771666
PubChem CID :
387447
Indice de Merck :
14: 1351
Número MDL :
MFCD09056737
SMILES :
CC(C)C[[email protected]](NC(=O)[[email protected]@H](CC1=CC=CC=C1)NC(=O)C2=NC=CN=C2)B(O)O

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Citaciones 1 a 10 de un total de 88

PMID: # 31015476  Lübbehüsen, C. et al. 2019. Sci Rep. 9: 6458.

PMID: # 31399560  Willbold, R.|Wirth, K.|Martini, T.|Sültmann, H.|Bolenz, C.|Wittig, R.| et al. 2019. Cell Death Dis. 10: 601.

PMID: # 31257577  Gomez-Puerto, MC. et al. 2019. J. Pathol.

PMID: # 29543923  Kocemba-Pilarczyk, KA.|Ostrowska, B.|Trojan, S.|Aslan, E.|Kusior, D.|Lasota, M.|Lenouvel, C.|Dulińska-Litewka, J.| et al. 2018. Acta Biochim. Pol. 65: 101-109.

PMID: # 29599781  Tucher, C.|Bode, K.|Schiller, P.|Claßen, L.|Birr, C.|Souto-Carneiro, MM.|Blank, N.|Lorenz, HM.|Schiller, M.| et al. 2018. Front Immunol. 9: 534.

PMID: # 30586869  Granato, M.|Gilardini Montani, MS.|Angiolillo, C.|D'Orazi, G.|Faggioni, A.|Cirone, M.| et al. 2018. Viruses. 11:

PMID: # 30224516  Alsanafi, M.|Kelly, SL.|Jubair, K.|McNaughton, M.|Tate, RJ.|Merrill, AH.|Pyne, S.|Pyne, NJ.| et al. 2018. Mol. Cell. Biol. 38:

PMID: # 29462804  Qin, XY. et al. 2018. Cell. Physiol. Biochem. 45: 1366-1376.

PMID: # 29669822  Song, X.|Lee, DH.|Dilly, AK.|Lee, YS.|Choudry, HA.|Kwon, YT.|Bartlett, DL.|Lee, YJ.| et al. 2018. Mol. Cancer Res. 16: 1077-1091.

PMID: # 28883123  Londino, JD. et al. 2017. The Biochemical journal. 474: 3543-3557.

Citaciones 1 a 10 de un total de 88
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