TAK-632

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Chemical Information

Product name：TAK-632	Purity：98% min
CAS NO：1228591-30-7	Solubility：DMSO : 100 mg/mL (180.34 mM)
Molecular Formula：C₂₇H₁₈F₄N₄O₃S	Package：Package according to customer requirements.
Molecular Weight：554.515	Storage：Store at -20℃

Quality control

COA

Remarks

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

Raf Inhibitors Related Products:

Vemurafenib; PLX-4720; Debrafenib; Regorafenib; GDC-0879; RAF265 (CHIR-265); AZ-628; SB590885; ZM 336372; B-Raf IN 1; AZ304; Dabrafenib Mesylate; RAF709; LY3009120; RO5126766; Doramapimod; MLN2480 ; GW5074

References

[1]. Okaniwa M, et al. 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.

[2]. Nakamura A, et al. Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. Cancer Res. 2013 Oct 11.