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5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide

Description In vitro In vivo
5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide
5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide structure
CAS No.
747412-49-3
Chemical Name:
5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide
Synonyms
AUY 922;VER 52296;VER-52296;NVP-AUY922;LuMinespib;AUY922, VER-52296;NVP-AUY922, >=98%;AUY922 (NVP-AUY922);NVP-AUY922 (Luminespib;Luminespib (NVP-AUY922)
CBNumber:
CB22489931
Molecular Formula:
C26H31N3O5
Formula Weight:
465.547
MOL File:
747412-49-3.mol

5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide Properties

Density 
1.234
CAS DataBase Reference
747412-49-3

5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide price More Price(2)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 10012698 NVP-AUY922 ≥98% 747412-49-3 5mg $125 2018-11-19 Buy
Cayman Chemical 10012698 NVP-AUY922 ≥98% 747412-49-3 10mg $200 2018-11-19 Buy

5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide Chemical Properties,Uses,Production

Description

Luminespib (AUY-922, NVP-AUY922) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 2.

In vitro

NVP-AUY922 inhibits proliferation of various human cancer cell lines in vitro, with an average GI50 of 9 nM. The IC50 values of NVP-AUY922 fall in the range of 2 to 40 nM in these gastric cancer cell lines. IC50 value for the BEAS-2B cells is 28.49 nM. Treatment with NVP-AUY922 does not influence the expression of HSP90, but expression of HSP70 gets elevated by NVP-AUY922 treatment. NVP-AUY922 increases the binding of HSP70 to HSP90. NVP-AUY922 causes p23 dissociation from the HSP90 complex and can then recruit HSP70 to the HSP90 complex. After the treatment with NVP-AUY922, expression of receptor tyrosine kinases including VEGFR1, 2, 3 and PDGFRɑ is decreased. A decrease is also noticed in the expression of Akt and phospho-Akt. Meanwhile, treatment with NVP-AUY922 causes decreased expression of HER-2 in NCI-N87 cells. NVP-AUY922 treatment results in binding of HSP90 to client proteins and setting them up as targets for degradation by the proteasome. NVP-AUY922 can influence cell growth by affecting multiple signaling pathways. In addition, treatment with the proteasome inhibitor, MG132, restores expression of thymidylate synthase, which is decreased by NVP-AUY922. NVP-AUY922 increases the expression of cleaved caspase-3 leading to apoptosis in HSC-2 cells.

In vivo

Treatment with NVP-AUY922 causes a robust antitumor response and inhibits p-Akt and VEGF expression in an HSC-2 xenograft model. In BT474, NVP-AUY922 shows complete loss of ERBB2 and substantial depletion of ERα, in addition to reductions in CDK4 and phospho-ERK1/2.

Uses

NVP-AUY 922 is a potent inhibitor of heat shock protein 90 (Hsp90) that prevents the proliferation of a range of human cancer cell lines. NVP-AUY 922 has been shown to enhance the radiation sensitivity of tumor cell lines under hypoxia.

Definition

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-(2,4-dihydroxy-5-isopropylphenyl)-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxylic acid with the amino group of ethylamine.

5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide Preparation Products And Raw materials

Raw materials

Preparation Products


5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide Suppliers

Global( 95)Suppliers
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Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19918 60
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24191 60
career henan chemical co
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Biochempartner
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Moltt Biocem Co., Ltd. +86-21-38682181 15900741819
+86-21-38682181 sales@moltt.com China 283 55
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2926 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76

View Lastest Price from 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-21 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide
747412-49-3
US $1.00 / KG 1G 98% 100KG career henan chemical co

747412-49-3(5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide)Related Search:


  • NVP-AUY922 - VER 52296 | Luminespib
  • AUY922, VER-52296
  • LuMinespib
  • Luminespib (AUY-922, NVP-AUY922)
  • AUY922,NVP-AUY-922,Luminespib
  • 5-(2,4-dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxamide
  • 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide AUY922 (NVP-AUY922)
  • Luminespib (NVP-AUY922)
  • NVP-AUY922, >=98%
  • NVP-AUY922, Luminespib, VER52296
  • 5-(2,4-Dihydroxy-5-isopropylphenyl)-N-ethyl-4-(4-(morpholinomethyl)phenyl)isoxazole-3-carboxam
  • NVP-AUY922 (Luminespib
  • 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide
  • NVP-AUY922
  • AUY 922
  • AUY922 (NVP-AUY922)
  • VER 52296
  • VER-52296
  • 747412-49-3
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Inhibitor
  • Antineoplastic
  • API
  • Potent and oral inhibitor of heat shock protein 90.
  • Aromatics
  • Heterocycles
  • Inhibitors
  • -
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