TAK-285

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP04168CAS No. ：871026-44-7Purity：98%

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CAS No.	871026-44-7	Cat. No.	BCP04168
Name	TAK-285
Synonyms	TAK 285;TAK285;
SMILES
Chemical Name
Formula	C26H25ClF3N5O3	M. Wt	547.96
Purity	98%	Storage	Store at 4-8°C
Description	Among the 34 kinases tested, TAK-285 only significantly inhibits HER4 with IC50 of 260 nM, slightly inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK, and Lyn B with IC50 of 1.1 μM, 5.7 μM, 4.2 μM, 1.7 μM, 2.4 μM, 4.7 μM, and 5.2 μM, respectively, and displays no activity against other kinases with IC50 of >10 μM. TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM.Compared with SYR127063 a potent inhibitor of HER2, TAK-285 displays similar in vitro potency against HER2 and EGFR. Compared with the full cytoplasmic domains of the wild-type proteins, the mutations and shortened boundaries used for structure determination of HER2-KD and EGFR-KD do not significantly change the inhibitory activity (IC50) of TAK-285. TAK-285 binds to the inactive conformation of EGFR, and shows a similar binding mode with lapatinib in the active site.