TAK-285

Name: TAK-285
SKU: A11236

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

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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	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.

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.

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