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TAK-733 CAS: 1035555-63-5

Category: Inhibitors
Product Name: TAK-733
Cat No: I000213
CAS No: 1035555-63-5
Synonyms: 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione
Molecular Formula: C17H15F2IN4O4
Molecular Weight: 504.2
SMILES: IC1=CC(F)=C(NC(C(C(N(C[C@@H](O)CO)C=N2)=O)=C2N3C)=C(F)C3=O)C=C1
InChI: None
InChIKey: RCLQNICOARASSR-SECBINFHSA-N
Solubility: DMSO: ≥ 33 mg/mL
Target: MEK1/2
IC50: 3.2 nM [1]
Storage: powder
CAS 1035555-63-5,TAK-733
  • Description

TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
IC50 Value: 3.2 nM [1]
Target: MEK1
in vitro: Sensitivity of cutaneous and uveal melanoma cell lines to TAK733 was investigated. five cutaneous melanoma cell lines wild type for mutations in NRAS, BRAF, GNAQand GNA11 and only one was highly sensitive to TAK733 with IC50s below 1 nM, while two were considered sensitive with IC50 less than 10 nM. All five uveal melanoma cell lines were sensitive to TAK733 with IC50 values below 10 nM, with three of them being highly sensitive. All these cell lines carried GNAQ or GNA11 driver mutations. Inhibition of oncogenic MAPK signaling through MEK1 and MEK2 by TAK733 results in antitumor activity in vitro against a large subset of melanoma cell lines[1].
in vivo: The in vivo antitumor activity of TAK-733, an investigational potent, selective, non-ATP-competitive allosteric inhibitor of MEK, in combination with alisertib, an investigational potent, selective, reversible, ATP-competitive inhibitor of Aurora A kinase, was examined in experimental human solid tumor xenograft models including NSCLC (NCI H23 [KRAS and LKB1 mutations]), CRC (SW620 [KRAS, APC, p53 mutations]), and pancreatic cancer (Panc 1 and Capan 1 [KRAS mutations] and BxPC-3 [No MAPK mutations]) models in immunocompromised mice[2].
Clinical trail: TAK733 clinical trail I is on the way for cancer(Melanoma, NSCLC, colorectal, breast cancer [3].

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


1:A phase I dose-escalation study of TAK-733, an investigational oral MEK inhibitor, in patients with advanced solid tumors. Adjei AA, LoRusso P, Ribas A, Sosman JA, Pavlick A, Dy GK, Zhou X, Gangolli E, Kneissl M, Faucette S, Neuwirth R, Bózon V.Invest New Drugs. 2017 Feb;35(1):47-58. doi: 10.1007/s10637-016-0391-2. Epub 2016 Sep 21. PMID: 27650277 Free PMC Article
2:MEK inhibitor, TAK-733 reduces proliferation, affects cell cycle and apoptosis, and synergizes with other targeted therapies in multiple myeloma. de la Puente P, Muz B, Jin A, Azab F, Luderer M, Salama NN, Azab AK.Blood Cancer J. 2016 Feb 26;6:e399. doi: 10.1038/bcj.2016.7. No abstract available. PMID: 26918363 Free PMC Article
3:Antitumor activity of a potent MEK inhibitor, TAK-733, against colorectal cancer cell lines and patient derived xenografts. Lieu CH, Klauck PJ, Henthorn PK, Tentler JJ, Tan AC, Spreafico A, Selby HM, Britt BC, Bagby SM, Arcaroli JJ, Messersmith WA, Pitts TM, Eckhardt SG.Oncotarget. 2015 Oct 27;6(33):34561-72. doi: 10.18632/oncotarget.5949. PMID: 26439693 Free PMC Article
4:Evaluation of the therapeutic efficacy of a MEK inhibitor (TAK-733) using ¹⁸F-fluorodeoxyglucose-positron emission tomography in the human lung xenograft model A549. Ishino S, Miyake H, Vincent P, Mori I.Ann Nucl Med. 2015 Aug;29(7):613-20. doi: 10.1007/s12149-015-0984-4. Epub 2015 May 27. PMID: 26014721 Free PMC Article
5:Antitumor activity of the MEK inhibitor TAK-733 against melanoma cell lines and patient-derived tumor explants. Micel LN, Tentler JJ, Tan AC, Selby HM, Brunkow KL, Robertson KM, Davis SL, Klauck PJ, Pitts TM, Gangolli E, Fabrey R, O'Connell SM, Vincent PW, Eckhardt SG.Mol Cancer Ther. 2015 Feb;14(2):317-25. doi: 10.1158/1535-7163.MCT-13-1012. Epub 2014 Nov 5. PMID: 25376610 Free PMC Article
6:Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Dong Q, Dougan DR, Gong X, Halkowycz P, Jin B, Kanouni T, O'Connell SM, Scorah N, Shi L, Wallace MB, Zhou F.Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. doi: 10.1016/j.bmcl.2011.01.071. Epub 2011 Jan 22. PMID: 21310613


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