HSP-990
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MedKoo CAT#: 205487

CAS#: 934343-74-5

Description: HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Hsp990 binds to and inhibits the activity of Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation.


Chemical Structure

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HSP-990
CAS# 934343-74-5

Theoretical Analysis

MedKoo Cat#: 205487
Name: HSP-990
CAS#: 934343-74-5
Chemical Formula: C20H18FN5O2
Exact Mass: 379.14445
Molecular Weight: 379.39
Elemental Analysis: C, 63.32; H, 4.78; F, 5.01; N, 18.46; O, 8.43

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 Same day
50.0mg USD 250.0 Same day
100.0mg USD 450.0 Same day
200.0mg USD 750.0 Same day
500.0mg USD 1750.0 Same day
1.0g USD 2850.0 Same day
2.0g USD 3950.0 Same day
5.0g USD 6950.0 Same day
10.0g USD 9650.0 Same day
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Synonym: HSP990; HSP-990; HSP 990; NVP HSP 990; NVP-HSP990; NVP HSP-990;

IUPAC/Chemical Name: (R)-2-amino-7-(4-fluoro-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one

InChi Key: WSMQUUGTQYPVPD-OAHLLOKOSA-N

InChi Code: InChI=1S/C20H18FN5O2/c1-10-18-16(26-20(22)23-10)9-15(25-19(18)27)12-7-6-11(21)8-13(12)14-4-3-5-17(24-14)28-2/h3-8,15H,9H2,1-2H3,(H,25,27)(H2,22,23,26)/t15-/m1/s1

SMILES Code: O=C1N[C@@H](C2=CC=C(F)C=C2C3=NC(OC)=CC=C3)CC4=NC(N)=NC(C)=C41

Appearance: white 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, not in water

Shelf Life: >2 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

Preparing Stock Solutions

The following data is based on the product molecular weight 379.39 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.

Recalculate based on batch purity %
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

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1: Spagnoletti G, Li Bergolis V, Piscazzi A, Giannelli F, Condelli V, Sisinni L, Bove G, Storto G, Landriscina M. Cyclin-dependent kinase 1 targeting improves sensitivity to radiation in BRAF V600E colorectal carcinoma cells. Tumour Biol. 2018 Apr;40(4):1010428318770957. doi: 10.1177/1010428318770957. PubMed PMID: 29663854.

2: Moriya C, Taniguchi H, Nagatoishi S, Igarashi H, Tsumoto K, Imai K. PRDM14 directly interacts with heat shock proteins HSP90α and glucose-regulated protein 78. Cancer Sci. 2018 Feb;109(2):373-383. doi: 10.1111/cas.13458. Epub 2017 Dec 28. PubMed PMID: 29178343; PubMed Central PMCID: PMC5797828.

3: Lee SL, Dempsey-Hibbert NC, Vimalachandran D, Wardle TD, Sutton PA, Williams JH. Re-examining HSPC1 inhibitors. Cell Stress Chaperones. 2017 Mar;22(2):293-306. doi: 10.1007/s12192-017-0774-0. Epub 2017 Mar 2. PubMed PMID: 28255900; PubMed Central PMCID: PMC5352602.

4: Palladino G, Notarangelo T, Pannone G, Piscazzi A, Lamacchia O, Sisinni L, Spagnoletti G, Toti P, Santoro A, Storto G, Bufo P, Cignarelli M, Esposito F, Landriscina M. TRAP1 regulates cell cycle and apoptosis in thyroid carcinoma cells. Endocr Relat Cancer. 2016 Sep;23(9):699-709. doi: 10.1530/ERC-16-0063. Epub 2016 Jul 15. PubMed PMID: 27422900.

5: Li L, An M, Shen H, Huang X, Yao X, Liu J, Zhu F, Zhang S, Chen S, He L, Zhang J, Zou Z, Jiang Y. The non-Geldanamycin Hsp90 inhibitors enhanced the antifungal activity of fluconazole. Am J Transl Res. 2015 Dec 15;7(12):2589-602. eCollection 2015. PubMed PMID: 26885259; PubMed Central PMCID: PMC4731659.

6: Spreafico A, Delord JP, De Mattos-Arruda L, Berge Y, Rodon J, Cottura E, Bedard PL, Akimov M, Lu H, Pain S, Kaag A, Siu LL, Cortes J. A first-in-human phase I, dose-escalation, multicentre study of HSP990 administered orally in adult patients with advanced solid malignancies. Br J Cancer. 2015 Feb 17;112(4):650-9. doi: 10.1038/bjc.2014.653. Epub 2015 Jan 27. PubMed PMID: 25625276; PubMed Central PMCID: PMC4333497.

7: Koul D, Yao J, Wan S, Yuan Y, Sulman E, Lang F, Yung WK, Colman H. Retraction: Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig 2-positive glioma tumor-initiating cells. Cancer Res. 2014 Nov 15;74(22):6731-2. doi: 10.1158/0008-5472.CAN-14-2966. PubMed PMID: 25398854; PubMed Central PMCID: PMC4381954.

8: McBride CM, Levine B, Xia Y, Bellamacina C, Machajewski T, Gao Z, Renhowe P, Antonios-McCrea W, Barsanti P, Brinner K, Costales A, Doughan B, Lin X, Louie A, McKenna M, Mendenhall K, Poon D, Rico A, Wang M, Williams TE, Abrams T, Fong S, Hendrickson T, Lei D, Lin J, Menezes D, Pryer N, Taverna P, Xu Y, Zhou Y, Shafer CM. Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990. J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4. PubMed PMID: 25368984.

9: Condelli V, Piscazzi A, Sisinni L, Matassa DS, Maddalena F, Lettini G, Simeon V, Palladino G, Amoroso MR, Trino S, Esposito F, Landriscina M. TRAP1 is involved in BRAF regulation and downstream attenuation of ERK phosphorylation and cell-cycle progression: a novel target for BRAF-mutated colorectal tumors. Cancer Res. 2014 Nov 15;74(22):6693-704. doi: 10.1158/0008-5472.CAN-14-1331. Epub 2014 Sep 19. PubMed PMID: 25239454.

10: Wachsberger PR, Lawrence YR, Liu Y, Rice B, Feo N, Leiby B, Dicker AP. Hsp90 inhibition enhances PI-3 kinase inhibition and radiosensitivity in glioblastoma. J Cancer Res Clin Oncol. 2014 Apr;140(4):573-82. doi: 10.1007/s00432-014-1594-6. Epub 2014 Feb 6. PubMed PMID: 24500492.

11: Aguilà M, Bevilacqua D, McCulley C, Schwarz N, Athanasiou D, Kanuga N, Novoselov SS, Lange CA, Ali RR, Bainbridge JW, Gias C, Coffey PJ, Garriga P, Cheetham ME. Hsp90 inhibition protects against inherited retinal degeneration. Hum Mol Genet. 2014 Apr 15;23(8):2164-75. doi: 10.1093/hmg/ddt613. Epub 2013 Dec 2. PubMed PMID: 24301679; PubMed Central PMCID: PMC3959821.

12: Zitzmann K, Ailer G, Vlotides G, Spoettl G, Maurer J, Göke B, Beuschlein F, Auernhammer CJ. Potent antitumor activity of the novel HSP90 inhibitors AUY922 and HSP990 in neuroendocrine carcinoid cells. Int J Oncol. 2013 Dec;43(6):1824-32. doi: 10.3892/ijo.2013.2130. Epub 2013 Oct 4. PubMed PMID: 24100469; PubMed Central PMCID: PMC3834873.

13: Gillis JL, Selth LA, Centenera MM, Townley SL, Sun S, Plymate SR, Tilley WD, Butler LM. Constitutively-active androgen receptor variants function independently of the HSP90 chaperone but do not confer resistance to HSP90 inhibitors. Oncotarget. 2013 May;4(5):691-704. PubMed PMID: 23674566; PubMed Central PMCID: PMC3742830.

14: Fu J, Koul D, Yao J, Wang S, Yuan Y, Colman H, Sulman EP, Lang FF, Yung WK. Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig2-positive glioma tumor-initiating cells. Cancer Res. 2013 May 15;73(10):3062-74. doi: 10.1158/0008-5472.CAN-12-2033. Epub 2013 Mar 14. Retraction in: Koul D, Yao J, Wan S, Yuan Y, Sulman E, Lang F, Yung WK, Colman H. Cancer Res. 2014 Nov 15;74(22):6731-2. PubMed PMID: 23492364; PubMed Central PMCID: PMC3655088.

15: Milanović D, Firat E, Grosu AL, Niedermann G. Increased radiosensitivity and radiothermosensitivity of human pancreatic MIA PaCa-2 and U251 glioblastoma cell lines treated with the novel Hsp90 inhibitor NVP-HSP990. Radiat Oncol. 2013 Feb 28;8:42. doi: 10.1186/1748-717X-8-42. PubMed PMID: 23448094; PubMed Central PMCID: PMC3599905.

16: Centenera MM, Gillis JL, Hanson AR, Jindal S, Taylor RA, Risbridger GP, Sutherland PD, Scher HI, Raj GV, Knudsen KE, Yeadon T; Australian Prostate Cancer BioResource, Tilley WD, Butler LM. Evidence for efficacy of new Hsp90 inhibitors revealed by ex vivo culture of human prostate tumors. Clin Cancer Res. 2012 Jul 1;18(13):3562-70. doi: 10.1158/1078-0432.CCR-12-0782. Epub 2012 May 9. PubMed PMID: 22573351.

17: Lamottke B, Kaiser M, Mieth M, Heider U, Gao Z, Nikolova Z, Jensen MR, Sterz J, von Metzler I, Sezer O. The novel, orally bioavailable HSP90 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases. Eur J Haematol. 2012 May;88(5):406-15. doi: 10.1111/j.1600-0609.2012.01764.x. Epub 2012 Mar 21. PubMed PMID: 22309072.

18: Stühmer T, Iskandarov K, Gao Z, Bumm T, Grella E, Jensen MR, Einsele H, Chatterjee M, Bargou RC. Preclinical activity of the novel orally bioavailable HSP90 inhibitor NVP-HSP990 against multiple myeloma cells. Anticancer Res. 2012 Feb;32(2):453-62. PubMed PMID: 22287732.

19: Menezes DL, Taverna P, Jensen MR, Abrams T, Stuart D, Yu GK, Duhl D, Machajewski T, Sellers WR, Pryer NK, Gao Z. The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Mol Cancer Ther. 2012 Mar;11(3):730-9. doi: 10.1158/1535-7163.MCT-11-0667. Epub 2012 Jan 12. PubMed PMID: 22246440.

20: Khong T, Spencer A. Targeting HSP 90 induces apoptosis and inhibits critical survival and proliferation pathways in multiple myeloma. Mol Cancer Ther. 2011 Oct;10(10):1909-17. doi: 10.1158/1535-7163.MCT-11-0174. Epub 2011 Aug 22. PubMed PMID: 21859842.

HSP-990

25.0mg / USD 150.0


Additional Information

Hsp90, upregulated in a variety of tumor cells, is a molecular chaperone that plays a key role in the conformational maturation, stability and function of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation and/or immune responses.