TAK-285

Catalog No.: A11236

HER2/EGFR inhibitor

TAK-285

TAK-285 Chemical Structure

CAS NO. 871026-44-7

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]

Availability: In stock

Package Price Qty
5 mg
$180.00
10 mg
$300.00
25 mg
$580.00
50 mg
$980.00
10mM * 1mL in DMSO
$256.00
Warning Products are for laboratory research use only. Not for human use. We do not sell to patients.

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
HER2IC50: 17nM
EGFR/HER1IC50: 23nM
HER4IC50: 260nM
MEK1IC50: 1.1μM
AuroraBIC50: 1.7μM
LCKIC50: 2.4μM
c-MetIC50: 4.2μM
CSKIC50: 4.7μM
LynBIC50: 5.2μM
MEK5IC50: 5.7μM
LynAIC50: >10μM
FAKIC50: >10μM
VEGFR1IC50: >10μM
VEGFR2IC50: >10μM
FGFR1IC50: >10μM
FGFR3IC50: >10μM
PDGFRαIC50: >10μM
PDGFRβIC50: >10μM
IRKIC50: >10μM
Tie-2IC50: >10μM
c-KitIC50: >10μM
IGF-1RIC50: >10μM
SrcIC50: >10μM
ASK1IC50: >10μM
TAK1IC50: >10μM
MEKK1IC50: >10μM
IKKβIC50: >10μM
JNK1IC50: >10μM
ERK1IC50: >10μM
p38αIC50: >10μM
PKAIC50: >10μM
PKCθIC50: >10μM
GSK-3βIC50: >10μM
B-RafIC50: >10μM
TTKIC50: >10μM
PLK1IC50: >10μM
In vitro DMSO 110 mg/mL (200.74 mM)
Water <1 mg/mL (<1 mM)
Ethanol 54 mg/mL (98.54 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.

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.

Chemical Properties

Catalog Num A11236
Actions Inhibitor
M. Wt 548.0
Formula C26H25ClF3N5O3
Solubility DMSO
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

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