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M-5602 Mubritinib, Free Base, >99%

[TAK-165]

M.W. 468.47

C25H23F3N4O2

[366017-09-6]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 25 mg/mL with warming; soluble in ethanol at 1.7 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 20-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• Mubritinib is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase.

• For inhibitory testing, HER2 was expressed in the following cell types:  bladder (HT1376, UMUC3, T24), kidney (ACHN), and prostate (DU145, LNCaP, LN-REC4).  IC50 values for mubritinib for the bladder cancer cell lines varied from 0.09 µM to greater than 25 µM.  All of the prostate cancer cell lines studied were sensitive (IC50 = 0.053-4.6 µM) to mubritinib, but ACHN cells were relatively less sensitive.  In the xenograft model, treatment with mubritinib for 14 days significantly inhibited growth of UMUC-3 (22.9%), ACHN (26.0%), and LN-REC4 (26.5%) when compared to control.  Nagasawa, J., et al.  "Novel HER2 selective tyrosine kinase inhibitor, TAK-165, inhibits bladder, kidney and androgen-independent prostate cancer in vitro and in vivo."  Int. J. Urol. 13:  587-592 (2006).

• Sold for laboratory or manufacturing purposes only; not for human, medical, 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.