Luminespib
Description In vitro In vivo- Product Name
- Luminespib
- CAS No.
- 747412-49-3
- Chemical Name
- Luminespib
- Synonyms
- CS-209;AUY 922;VER-52296;VER 52296;NVP-AUY922;LuMinespib;NVP-AUY922-NX;AUY922, VER-52296;NVP-AUY922, >=98%;AUY922 (NVP-AUY922)
- CBNumber
- CB22489931
- Molecular Formula
- C26H31N3O5
- Formula Weight
- 465.54
- MOL File
- 747412-49-3.mol
Luminespib Property
- Melting point:
- 180-184°C
- Boiling point:
- 640.1±55.0 °C(Predicted)
- Density
- 1.234
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (>25 mg/ml)
- form
- solid
- pka
- 8.47±0.48(Predicted)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
- CAS DataBase Reference
- 747412-49-3
Safety
- HS Code
- 2934999090
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
N-Bromosuccinimide Price
- Product number
- 10012698
- Product name
- NVP-AUY922
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $153
- Updated
- 2024/03/01
- Product number
- 10012698
- Product name
- NVP-AUY922
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $243
- Updated
- 2024/03/01
- Product number
- 018620
- Product name
- NVP-AUY 922
- Packaging
- 10mg
- Price
- $496
- Updated
- 2021/12/16
- Product number
- N925650
- Product name
- NVP-AUY922
- Packaging
- 100mg
- Price
- $1240
- Updated
- 2021/12/16
- Product number
- CS-0136
- Product name
- Luminespib
- Purity
- 99.81%
- Packaging
- 500mg
- Price
- $1320
- Updated
- 2021/12/16
Luminespib Chemical Properties,Usage,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.
Description
Hsp90 is a molecular chaperone of many different kinases, transcription factors, and hormone receptors involved in signal transduction, cell cycle regulation, and apoptosis. In addition to its important function in normal cell homeostasis, a high affinity form of Hsp90 is prevalent in tumor cells. Hsp90 inhibition has been associated with the degradation of oncogenic client proteins. NVP-
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. Potent Hedgehog inhibitor.
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.
target
HSP90α
References
Brough et al. (2008), 4,5-Diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer; Med. Chem. 51 196 Eccles et al. (2008), NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis; Cancer Res. 68 2850 Massey et al. (2010), Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor; Cancer Ther. 5 1807 Song et al. (2020), HSP90A inhibition promotes anti-tumor immunity by reversing multi-modal resistance and stem-like property of immune-refractory tumors; Commun. 11 562 Schwab and Multhoff (2022), A Low Membrane Hsp70 Expression in Tumor Cells With Impaired Lactate Metabolism Mediates Radiosensitization by NVP-AUY922; Oncol. 12 861266 Djuzenova et al. (2012), Hsp90 inhibitor NVP-AUY922 enhances radiation sensitivity of tumor cells lines under hypoxia; Cancer Biol. Ther. 13 425 Schilling et al. (2015), Sensitizing tumor cells to radiation by targeting the heat shock response; Cancer Lett. 360 294
Luminespib Preparation Products And Raw materials
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View Lastest Price from Luminespib manufacturers
- Product
- luminespib 747412-49-3
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-26
- Product
- 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide 747412-49-3
- Price
- US $1.00/KG
- Min. Order
- 1G
- Purity
- 98%
- Supply Ability
- 100KG
- Release date
- 2018-08-21