TAK-632 is a potent pan-RAF inhibitor with favorable in vitro activity (BRAF(V600E) IC50, 2.4 nM; BRAF(wt), 8.3 nM; CRAF, 1.4 nM; pMEK (A375) IC50, 12 nM; pMEK (HMVII), 49 nM; V/B ratio. In addition, TAK-632 was shown preclinically to be a selective kinase inhibitor targeting pan-RAF kinase activity by testing against a panel of kinases. In both A375 (BRAFV600E) and HMVII (NRASQ61K) xenograft models in rats, TAK-632 demonstrated regressive antitumor efficacy by twice daily, 14-day repetitive administration without significant body weight loss

MedKoo Cat#: 406295 Name: TAK-632 CAS#: 1228591-30-7 Chemical Formula: C27H18F4N4O3S Exact Mass: 554.10357 Molecular Weight: 554.51 Elemental Analysis: C, 58.48; H, 3.27; F, 13.70; N, 10.10; O, 8.66; S, 5.78

Synonym: TAK632, TAK 632, TAK-632

IUPAC/Chemical Name: N-(7-cyano-6-(4-fluoro-3-(2-(3-(trifluoromethyl)phenyl)acetamido)phenoxy)benzo[d]thiazol-2-yl)cyclopropanecarboxamide

InChi Key: OJFKUJDRGJSAQB-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H18F4N4O3S/c28-19-7-6-17(12-21(19)33-23(36)11-14-2-1-3-16(10-14)27(29,30)31)38-22-9-8-20-24(18(22)13-32)39-26(34-20)35-25(37)15-4-5-15/h1-3,6-10,12,15H,4-5,11H2,(H,33,36)(H,34,35,37)

SMILES Code: O=C(C1CC1)NC(S2)=NC3=C2C(C#N)=C(OC4=CC(NC(CC5=CC=CC(C(F)(F)F)=C5)=O)=C(F)C=C4)C=C3

Technical Data

Appearance: White solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Certificate of Analysis: View CoA: current batch, Lot#CRB40226

QC Data: View QC data: current batch, Lot#CRB40226

Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)

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).

Harmonized System Code: 293490

References

1: Nakamura A, Arita T, Tsuchiya S, Donelan J, Chouitar J, Carideo E, Galvin K, Okaniwa M, Ishikawa T, Yoshida S. Antitumor Activity of the Selective Pan-RAF Inhibitor TAK-632 in BRAF Inhibitor-Resistant Melanoma. Cancer Res. 2013 Dec 1;73(23):7043-55. doi: 10.1158/0008-5472.CAN-13-1825. Epub 2013 Oct 11. PubMed PMID: 24121489.

2: Okaniwa M, Hirose M, Arita T, Yabuki M, Nakamura A, Takagi T, Kawamoto T, Uchiyama N, Sumita A, Tsutsumi S, Tottori T, Inui Y, Sang BC, Yano J, Aertgeerts K, Yoshida S, Ishikawa T. Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. J Med Chem. 2013 Aug 22;56(16):6478-94. doi: 10.1021/jm400778d. Epub 2013 Aug 1. PubMed PMID: 23906342.

3: Sung SH, Jeon SW, Son HS, Kim SK, Jung MK, Cho CM, Tak WY, Kweon YO. Factors predictive of risk for complications in patients with oesophageal foreign bodies. Dig Liver Dis. 2011 Aug;43(8):632-5. doi: 10.1016/j.dld.2011.02.018. Epub 2011 Apr 3. PubMed PMID: 21466978.

4: Biró E, Nieuwland R, Tak PP, Pronk LM, Schaap MC, Sturk A, Hack CE. Activated complement components and complement activator molecules on the surface of cell-derived microparticles in patients with rheumatoid arthritis and healthy individuals. Ann Rheum Dis. 2007 Aug;66(8):1085-92. Epub 2007 Jan 29. PubMed PMID: 17261534; PubMed Central PMCID: PMC1954699.