TAK-285

Catalog No. A11236

TAK-285是一种研究性的HER2/EGFR抑制剂，可在具有完整血脑屏障 (BBB) 的大鼠中穿透CNS。TAK-285对HER2和EGFR激酶具有抑制活性，HER2和EGFR的IC50值分别为17 nmol/L (95％CI 12-24)和23 nmol/L (95％CI 18-30)。

Technical details

Catalog Num	A11236
M. Wt	548.0
Formula	C26H25ClF3N5O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	871026-44-7
Synonyms	TAK285
SMILES	CC(C)(CC(=O)NCCN1C=CC2=C1C(=NC=N2)NC3=CC(=C(C=C3)OC4=CC=CC(=C4)C(F)(F)F)Cl)O

Biological Activity

Targets

Target	Value
HER2	IC50: 17nM
EGFR/HER1	IC50: 23nM
HER4	IC50: 260nM
MEK1	IC50: 1.1μM
AuroraB	IC50: 1.7μM
LCK	IC50: 2.4μM
c-Met	IC50: 4.2μM
CSK	IC50: 4.7μM
LynB	IC50: 5.2μM
MEK5	IC50: 5.7μM
LynA	IC50: >10μM
FAK	IC50: >10μM
VEGFR1	IC50: >10μM
VEGFR2	IC50: >10μM
FGFR1	IC50: >10μM
FGFR3	IC50: >10μM
PDGFRα	IC50: >10μM
PDGFRβ	IC50: >10μM
IRK	IC50: >10μM
Tie-2	IC50: >10μM
c-Kit	IC50: >10μM
IGF-1R	IC50: >10μM
Src	IC50: >10μM
ASK1	IC50: >10μM
TAK1	IC50: >10μM
MEKK1	IC50: >10μM
IKKβ	IC50: >10μM
JNK1	IC50: >10μM
ERK1	IC50: >10μM
p38α	IC50: >10μM
PKA	IC50: >10μM
PKCθ	IC50: >10μM
GSK-3β	IC50: >10μM
B-Raf	IC50: >10μM
TTK	IC50: >10μM
PLK1	IC50: >10μM

Solubility *

In vitro	DMSO	97 mg/mL (177.02 mM)
	Water	Insoluble
	Ethanol	48 mg/mL (87.59 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	18.25 mL	91.24 mL	182.48 mL
0.5 mM	3.65 mL	18.25 mL	36.5 mL
1 mM	1.82 mL	9.12 mL	18.25 mL
5 mM	0.36 mL	1.82 mL	3.65 mL

*The above data is based on the productmolecular weight 548.0 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

References

1. Shinji Takagi, Hiroshi Banno, Akira Hayashi, Toshiya Tamura, Tomoyasu Ishikawa, Yoshikazu Ohta., HER2 and HER3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational EGFR/HER2 kinase inhibitor TAK-285. Oncoscience, 2014. 1(3): p. 196-204.