BEZ235CAS: 915019-65-7
MF: C30H23N5O
MW: 469.55
A dual PI3K and mTOR inhibitor.

BEZ235 (CAS 915019-65-7)

BEZ235 | CAS 915019-65-7 is rated 5.0 out of 5 by 1.
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Synonym: Dactolisib; NVP-BEZ235
Application: A dual PI3K and mTOR inhibitor
CAS Number: 915019-65-7
Purity: ≥97%
Molecular Weight: 469.55
Molecular Formula: C30H23N5O
* Refer to Certificate of Analysis for lot specific data (including water content).
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BEZ235 is a PI 3-kinase (PI3K) tyrosine kinase inhibitor and shows dual PI3K/mTOR inhibition (IC50 = 4, 5, 7 and 75 nM for PI 3-Kα, -γ, -δ, and -β, respectively). BEZ235 showed high target specificity and demonstrated antiproliferative activity against tumor cell lines in animal models of cancer. BEZ235 is an mTOR Complex 1 and mTOR Complex 2 catalytic inhibitor. BEZ235 also inhibits ATR (IC50 = 21nM).


References

1. Maira, S.M. et al. 2008. Mol. Cancer Ther. 7(7): 1851-1863. PMID: 18606717
2. Chiarini, F. et al. 2010. Cancer Res. 70(20): 8097-8107. PMID: 20876803
3. Cho, D.C. et al. 2010. Clin. Cancer Res. 16(14): 3628-3638. PMID: 20606035
4. Elliott, N.E. et al. 2011. Blood. 118(14): 3911-3921. PMID: 21821710
5. Roulin, D. et al. 2011. Mol. Cancer. 10 : 90. PMID: 21791089
6. Toledo, L.I. et al. 2011. Nat. Struct. Mol. Biol. 18(6): 721-727. PMID: 21552262
7. Roper, J. et al. 2011. PLoS ONE. 6(9): e25132. PMID: 21966435
8. Pei, Y. et al. 2012. Cancer Cell. 21(2): 155-167. PMID: 22340590
9. Zhang, Y. et al. 2012. J. Cell. Physiol. 227(1): 35-43. PMID: 21412767
10. Wilson, T.R. et al. 2012. Nature. 487(7408): 505-509. PMID: 22763448
11. Shoji, K. et al. 2012. PLoS ONE. 7(5): e37431. PMID: 22662154
12. Fallahi-Sichani, M. et al. 2013. Nat. Chem. Biol. 9(11): 708-714. PMID: 24013279
13. Grasso, C.S. et al. 2015. Nat. Med. 21(6): 555-559. PMID: 25939062

Physical State :
Solid
Solubility :
Soluble in chloroform (1 mg/ml), 1-methyl-2-pyrrolidnone (2 mg/mL at 75 °C), DMSO (1.33 mg/mL), and DMF (10 mg/mL at 75 °C).
Storage :
Store at -20° C
Melting Point :
288-289° C
Boiling Point :
701.03° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
PI3K p110α: IC50 = 4 nM; PI3K p110γ: IC50 = 5 nM; mTOR: IC50 = 6 nM; PI3K p110δ: IC50 = 7 nM; ATR: IC50 = 21 nM
Ki Data :
CLK4: Ki= 31.62 nM (human); GC kinase: Ki= 50.12 nM (human); Chk1: Ki= 50.12 nM (human); c-Fms/CSF-1R: Ki= 0.32 µM (human); LTK: Ki= 0.32 µM (human)
pK Values :
pKb: 6.41 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11977753
MDL Number :
MFCD10565944
SMILES :
CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

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Certificate of Analysis

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BEZ235  Product Citations

See how others have used BEZ235. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 29533781  Morita, M.|Sato, T.|Nomura, M.|Sakamoto, Y.|Inoue, Y.|Tanaka, R.|Ito, S.|Kurosawa, K.|Yamaguchi, K.|Sugiura, Y.|Takizaki, H.|Yamashita, Y.|Katakura, R.|Sato, I.|Kawai, M.|Okada, Y.|Watanabe, H.|Kondoh, G.|Matsumoto, S.|Kishimoto, A.|Obata, M.|Matsumoto, M.|Fukuhara, T.|Motohashi, H.|Suematsu, M.|Komatsu, M.|Nakayama, KI.|Watanabe, T.|Soga, T.|Shima, H.|Maemondo, M.|Tanuma, N.| et al. 2018. Cancer Cell. 33: 355-367.e7.

PMID: # 27737796  Hamunyela, RH. et al. 2017. Toxicol In Vitro. 38: 117-123.

PMID: # 28650474  Zimmermannova, O. et al. 2017. Oncogene. 36: 5985-5994.

PMID: # 26728896  ur Rasool, R. et al. 2016. Sci Rep. 6: 18800.

PMID: # 26927829  Surovtseva, YV. et al. 2016. J. Am. Chem. Soc. 138: 3844-55.

Citations 1 to 5 of 5 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. BEZ235, sc-364429, is in white to off-white powder form.
Answered by: Chemical Support 4
Date published: 2017-04-28
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Rated 5 out of 5 by from Popescu et al Popescu et al. (PubMed ID 26339347) used BEZ235 to inhibit PI3K/Akt/mTOR signaling pathways of gliobastoma cells in vitro and found this to stimulate early activation of caspase 3, 8 and 9. -SCBT Publication Review
Date published: 2015-03-16
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