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NVP-BEP800

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NVP-BEP800 Basic information

Product Name:
NVP-BEP800
Synonyms:
  • NVP-BEP800
  • 2-amino-4-(2,4-dichloro-5-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
  • NVP-BEP800;2-AMINO-4-(2,4-DICHLORO-5-(2-(PYRROLIDIN-1-YL)ETHOXY)PHENYL)-N-ETHYLTHIENO[2,3-D]PYRIMIDINE-6-CARBOXAMIDE
  • 2-Amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
  • VER82576
  • VER-82576
  • 2-Amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide NVP-BEP 800
  • NVP-BEP 800 2-Amino-4-[2,4-dichloro-5-[2-(1-pyrrolidinyl)ethoxy]phenyl]-N-ethylthieno[2,3-d]pyrimidine-6-carboxamide
CAS:
847559-80-2
MF:
C21H23Cl2N5O2S
MW:
480.41
Product Categories:
  • Inhibitor
  • apis
  • Inhibitors
Mol File:
847559-80-2.mol
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NVP-BEP800 Chemical Properties

Density 
1.396
storage temp. 
Store at -20°C
solubility 
insoluble in H2O; ≥16 mg/mL in EtOH with gentle warming; ≥24.7 mg/mL in DMSO with gentle warming and ultrasonic
form 
Powder
pka
13.25±0.46(Predicted)
color 
White to off-white
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NVP-BEP800 Usage And Synthesis

Uses

NVP-BEP 800 is a Hsp90 inhibitor which ehibits anti-proliferative effects against cancer cell lines with high expression level of Hsp90.

Biological Activity

nvp-bep800 is a fully synthetic, orally bioavailable inhibitor of hsp90 with ic50 value of 58nm [1].nvp-bep800 binds to the n-terminal atp-binding pocket of hsp90. in a competitive binding fluorescence polarization assay, nvp-bep800 inhibits hsp90β with ic50 value of 58nm. and to other 20 protein kinases, nvp-bep800 shows a ic50 of >10μm. in bt-474 cells and a375 cells, nvp-bep800 causes the hsp90-p23 dissociation and client protein degradation (erbb2) as well as the reduction of client protein phosphorylation (phospho-akt). degradation of these oncogenic client proteins results in tumor cell growth arrest and death. nvp-bep800 inhibits proliferation of tumor cells with an average gi50 of 245nm. and in 46 primary human tumors including small cell lung, mammary cancer and melanoma, the mean ic50 is 750nm. additionally, treatment of nvp-bep800 induces apoptosis in human breast cancer cell lines. the antitumor efficacy of nvp-bep800 is also observed with a dose of 15 or 30 mg/kg/d in a375 xenograft-bearing mice as well as in bt-474 breast cancer xenografts [1].

target

Hsp90β

References

[1] massey aj, schoepfer j, brough pa, brueggen j, chène p, drysdale mj, pfaar u, radimerski t, ruetz s, schweitzer a, wood m, garcia-echeverria c, jensen mr. preclinical antitumor activity of the orally available heat shock protein 90 inhibitor nvp-bep800. mol cancer ther. 2010 apr;9(4):906-19.

NVP-BEP800Supplier

Shanghai Boyle Chemical Co., Ltd.
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sales@boylechem.com
Jinan Trio PharmaTech Co., Ltd.
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+86 (531) 88811783
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sales@trio-pharmatech.com (International market)
China Langchem Inc.
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0086-21-58956006
Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988