A-2345 AZD8055, Free Base, >99%

Synonyms : [CCG-168]

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  • 5 mg
  • 37
  • 34
  • 29
  • 5,800
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  • 10 mg
  • 49
  • 45
  • 38
  • 7,600
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  • 25 mg
  • 85
  • 78
  • 66
  • 13,200
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  • 50 mg
  • 115
  • 105
  • 90
  • 17,900
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  • 100 mg
  • 184
  • 169
  • 144
  • 28,600
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  • 200 mg
  • 332
  • 305
  • 261
  • 51,700
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  • M.W. 465.54
  • C25H31N5O4
  • [1009298-09-2]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 50 mg/mL; soluble in ethanol at 20 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM; buffers, serum, or other additives may increase or decrease the aqueous solubilit. Disposal: A.

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  • AZD8055 is a novel ATP-competitive and selective inhibitor of mammalian target of rapamycin (mTOR) kinase with an IC50 value of 0.8 nM. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1, mTORC2 substrate AKT, and downstream proteins. AZD8055 fully inhibits the rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 and results in significant inhibition of cap-dependent translation. AZD8055 potently inhibits proliferation and induces autophagy in vitro, and causes significant growth inhibition and/or regression in xenografts in vivo. Chresta, C.M., et al. "AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity." Cancer Res. 70: 288-298 (2010).
  • The combination of the MAPK extracellular signal-regulated kinase (MEK1/2) inhibitor selumetinib (AZD6244, please see Cat. No. S-4490, Selumetinib, Free Base) with the dual mTORC1 and mTORC2 inhibitor AZD8055 were used in nude mouse xenograft models of human lung adenocarcinoma (non-small cell lung cancers) and colorectal carcinoma. The treatment was well tolerated and showed improved antitumor efficacy when compared to the respective monotherapies. The reciprocal pathway inhibition from the combination group was associated with increased apoptosis and Bcl-2 interacting mediator of cell death (Bim) expression in tumor tissue. Holt, S.V., et al. "Enhanced apoptosis and tumor growth suppression elicited by combination of MEK (selumetinib) and mTOR kinase inhibitors (AZD8055)." Cancer Res. 72: 1804-1813 (2012).
  • The mTOR molecular signaling pathway plays a critical role in cerebral vasospasm following subarachnoid hemorrhage (SAH). AZD8055 significantly inhibited the level and expression of key mTOR signaling pathway molecules including mTOR, P70S6K1, 4E-BP1 and PCNA, and thus inhibited the mTOR pathway, thus suggesting that AZD8055 has the potential to treat vasospasm following SAH. Zhang, W., et al. "Mammalian target of rapamycin (mTOR) inhibition reduces cerebral vasospasm following a subarachnoid hemorrhage injury in canines." Exp. Neurol. 233: 799-806 (2012).
  • AZD8055 inhibited both mTORC1 and mTORC2 signaling in acute myeloid leukemia (AML) in mice. AZD8055 significantly reduced the tumor growth and markedly increased the survival of AML transplanted mice without apparent toxicity. Willems, L., et al. "The dual mTORC1 and mTORC2 inhibitor AZD8055 has anti-tumor activity in acute myeloid leukemia." Leukemia 26: 1195-1202 (2012).
  • AZD8055 blocked the chemotherapy-induced cell death promoted by ectopic wild-type p62. Huang, S., et al. "Inhibition of mTOR kinase by AZD8055 can antagonize chemotherapy-induced cell death through autophagy induction and down-regulation of p62/sequestosome 1." J. Biol. Chem. 286: 40002-40012 (2011).
  • The combination of mTOR kinase inhibitor AZD8055 and histone deacetylase inhibitor SAHA (vorinostat, please see Cat. No. V-8477, Vorinostat) almost completely inhibited tumor growth of hepatocellular carcinoma (HCC) by upregulating Bim and abrogating AKT. However, either agent alone demonstrated only 30% inhibition in primary HCC xenografts. Shao, H., et al. "Dual targeting of mTORC1/C2 complexes enhances histone deacetylase inhibitor-mediated anti-tumor efficacy in primary HCC cancer in vitro and in vivo." J. Hepatol. 56: 176-183 (2012).
  • Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumors were tested in Western patients and Japanese patients. The maximum tolerated dose for AZD8055 was 90 mg BID. Aside from elevated transaminases, the drug had an acceptable toxicity profile. Naing, A., et al. "Safety, tolerability, pharmacokinetics and pharmacodynamics of AZD8055 in advanced solid tumours and lymphoma." Br. J. Cancer 107: 1093-1099 (2012). Asahina H., et al. "Safety and tolerability of AZD8055 in Japanese patients with advanced solid tumors; a dose-finding phase I study." Invest. New Drugs 31: 677-684 (2013).
  • Related CAS numbers: 1201799-05-4 for the fumarate salt form of AZD8055.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.