WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H573547
CAS#: 747412-64-2 (HCl)
Description: Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.
Hodoodo Cat#: H573547
Name: Luminespib HCl
CAS#: 747412-64-2 (HCl)
Chemical Formula: C27H34ClN3O5
Exact Mass: 479.24
Molecular Weight: 516.035
Elemental Analysis: C, 62.84; H, 6.64; Cl, 6.87; N, 8.14; O, 15.50
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Related CAS #: 747412-49-3 747412-64-2 (HCl) 1051919-26-6 (mesylate hydrate) 1051919-21-1 (mesylate)
Synonym: Luminespib HCl; AUY922; AUY-922; AUY 922; NVP AUY922; NVP AUY-922; VER52296 ; VER-52296 ; VER 52296 ; Luminespib
IUPAC/Chemical Name: 3-Isoxazolecarboxamide, 5-(5-(1,1-dimethylethyl)-2,4-dihydroxyphenyl)-N-ethyl-4-(4-(4-morpholinylmethyl)phenyl)- hydrochloride
InChi Key: AYYGBRAFXWJXCJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C27H33N3O5.ClH/c1-5-28-26(33)24-23(18-8-6-17(7-9-18)16-30-10-12-34-13-11-30)25(35-29-24)19-14-20(27(2,3)4)22(32)15-21(19)31;/h6-9,14-15,31-32H,5,10-13,16H2,1-4H3,(H,28,33);1H
SMILES Code: O=C(C1=NOC(C2=CC(C(C)(C)C)=C(O)C=C2O)=C1C3=CC=C(CN4CCOCC4)C=C3)NCC.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 516.04 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Felip E, Barlesi F, Besse B, Chu Q, Gandhi L, Kim SW, Carcereny E, Sequist LV, Brunsvig P, Chouaid C, Smit EF, Groen HJM, Kim DW, Park K, Avsar E, Szpakowski S, Akimov M, Garon EB. Phase 2 Study of the HSP-90 Inhibitor AUY922 in Previously Treated and Molecularly Defined Patients with Advanced Non-Small Cell Lung Cancer. J Thorac Oncol. 2018 Apr;13(4):576-584. doi: 10.1016/j.jtho.2017.11.131. Epub 2017 Dec 13. PubMed PMID: 29247830.
2: Wang CY, Guo ST, Croft A, Yan XG, Jin L, Zhang XD, Jiang CC. BAG3-dependent expression of Mcl-1 confers resistance of mutant KRAS colon cancer cells to the HSP90 inhibitor AUY922. Mol Carcinog. 2018 Feb;57(2):284-294. doi: 10.1002/mc.22755. Epub 2017 Nov 14. PubMed PMID: 29068469.
3: Lian J, Lin D, Xie X, Xu Y, Xu L, Meng L, Zhu Y. NVP-AUY922, a novel HSP90 inhibitor, inhibits the progression of malignant pheochromocytoma in vitro and in vivo. Onco Targets Ther. 2017 Apr 19;10:2219-2226. doi: 10.2147/OTT.S130236. eCollection 2017. PubMed PMID: 28458565; PubMed Central PMCID: PMC5403128.
4: Kosovec JE, Zaidi AH, Kelly LA, Rotoloni CL, Vytlacil C, DiCarlo C, Matsui D, Komatsu Y, Boyd NH, Omstead A, Kolano EL, Biederman RW, Finley G, Silverman JF, Landreneau RJ, Jobe BA. Preclinical Study of AUY922, a Novel Hsp90 Inhibitor, in the Treatment of Esophageal Adenocarcinoma. Ann Surg. 2016 Aug;264(2):297-304. doi: 10.1097/SLA.0000000000001467. PubMed PMID: 26445473.
