Biological Activity
TAK-285 is an investigational HER2/EGFR inhibitor that penetrates the CNS in Rats with an Intact Blood Brain Barrier (BBB). TAK-285 has inhibitory activity against HER2 and EGFR kinases with IC50 values for HER2 and EGFR of 17 nmol/L (95% CI 12-24) and 23 nmol/L (95% CI 18-30), respectively.[1]
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 |
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. |
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.
Catalog Num | A11236 |
---|---|
Actions | Inhibitor |
CAS No. | 871026-44-7 |
Formula | C26H25ClF3N5O3 |
M. Wt | 548.0 |
Purity | >98% |
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 |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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.
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