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TAK-285

HER2/EGFR inhibitor

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Catalog No. A11236

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
TAK-285 5mg A11236-5
€171.00
TAK-285 10mg A11236-10
€285.00
TAK-285 25mg A11236-25
€551.00
TAK-285 50mg A11236-50
€931.00
TAK-285 10mM * 1mL in DMSO A11236-10mM-D
€243.20

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

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]

TAK-285

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Chemical Information

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 code CC(C)(CC(=O)NCCN1C=CC2=C1C(=NC=N2)NC3=CC(=C(C=C3)OC4=CC=CC(=C4)C(F)(F)F)Cl)O
Chemical Name N-(2-(4-((3-chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide

Biological Activity

Description
 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

Solubility

Solubility (25°C)* 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 182.48mL
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.

Cat. No.

Product NameSolubility(mg/mL)
WaterDMSOEthanol
A10043 AEE788 <1 mg/mL 88 mg/mL <1 mg/mL
A11022 AG-1478 (Tyrphostin AG-1478) <1 mg/mL 25 mg/mL 13 mg/mL
A10047 AG 490 <1 mg/mL 59 mg/mL 6 mg/mL
A11027 ARRY-380 <1 mg/mL 114 mg/mL <1 mg/mL
A11158 ARRY334543 <1 mg/mL 6 mg/mL <1 mg/mL
A11155 AST-1306 <1 mg/mL 124 mg/mL <1 mg/mL
A10116 AZD8931 <1 mg/mL 40 mg/mL <1 mg/mL
A11334 BIBX 1382 50 mg/mL 50 mg/mL N/A
A11209 Lenalidomide (CC-5013) <1 mg/mL 113 mg/mL 20 mg/mL
A10743 BMS 599626 (AC480) <1 mg/mL 55 mg/mL <1 mg/mL
A10211 Canertinib (CI-1033) <1 mg/mL 2 mg/mL 9 mg/mL
A10210 Chrysophanic acid (Chrysophanol) <1 mg/mL <1 mg/mL <1 mg/mL
A10242 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
A10362 Erlotinib hydrochloride <1 mg/mL 3 mg/mL <1 mg/mL
A10422 Gefitinib (Iressa) <1 mg/mL 89 mg/mL 4 mg/mL
A10514 Lapatinib Ditosylate <1 mg/mL 185 mg/mL <1 mg/mL
A10612 Mubritinib (TAK 165) 13 mg/mL <1 mg/mL <1 mg/mL
A10638 Neratinib (HKI-272) 2 mg/mL <1 mg/mL <1 mg/mL
A10678 OSI-420 83 mg/mL 2 mg/mL <1 mg/mL
A10702 PD153035 (HCl salt) <1 mg/mL <1 mg/mL <1 mg/mL
A10706 Pelitinib (EKB-569) <1 mg/mL 13 mg/mL <1 mg/mL
A11051 PF299804 <1 mg/mL 19 mg/mL <1 mg/mL
A11236 TAK-285 <1 mg/mL 110 mg/mL 54 mg/mL
A10053 Tyrphostin AG 879 36 mg/mLtd <1 mg/mL 3 mg/mL
A10990 WZ3146 <1 mg/mL 93 mg/mL <1 mg/mL
A10991 WZ4002 13 mg/mL <1 mg/mL <1 mg/mL
A10992 WZ8040 96 mg/mL <1 mg/mL 3 mg/mL

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