Luminespib
- CAS No.
- 747412-49-3
- Chemical Name:
- Luminespib
- Synonyms
- CS-209;AUY 922;VER-52296;VER 52296;LuMinespib;NVP-AUY922;NVP-AUY922-NX;AUY922, VER-52296;NVP-AUY922, >=98%;AUY922 (NVP-AUY922)
- CBNumber:
- CB22489931
- Molecular Formula:
- C26H31N3O5
- Molecular Weight:
- 465.54
- MDL Number:
- MFCD14635361
- MOL File:
- 747412-49-3.mol
- MSDS File:
- SDS
| 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 |
| FDA UNII | C6V1DAR5EB |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P271-P280 | |||||||||
| HS Code | 2934999090 | |||||||||
| NFPA 704 |
|
Luminespib price More Price(42)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 10012698 | NVP-AUY922 ≥98% | 747412-49-3 | 5mg | $153 | 2024-03-01 | Buy |
| Cayman Chemical | 10012698 | NVP-AUY922 ≥98% | 747412-49-3 | 10mg | $243 | 2024-03-01 | Buy |
| Usbiological | 018620 | NVP-AUY 922 | 747412-49-3 | 10mg | $496 | 2021-12-16 | Buy |
| TRC | N925650 | NVP-AUY922 | 747412-49-3 | 100mg | $1240 | 2021-12-16 | Buy |
| ChemScene | CS-0136 | Luminespib 99.81% | 747412-49-3 | 500mg | $1320 | 2021-12-16 | Buy |
Luminespib 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.
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
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49391 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Hubei Ipure Biology Co., Ltd | +8613367258412 | ada@ipurechemical.com | China | 10326 | 58 |
View Lastest Price from Luminespib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2021-07-02 | luminespib
747412-49-3
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd | |
![5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide pictures](https://img.chemicalbook.com/ProductImageEN/2018-8/Small/f4935d30-a38e-4bef-be96-57c345a031ed.jpg) |
2019-07-06 | 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 |
-
- luminespib
747412-49-3
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
-
- 5-[2,4-Dihydroxy-5-isopropylphenyl]-N-ethyl-4-[4-(4-morpholinylmethyl)phenyl]-3-isoxazolecarboxamide
747412-49-3
- US $1.00 / KG
- 98%
- Career Henan Chemical Co