1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. TAK-285

TAK-285 

Cat. No.: HY-15196 Purity: 99.16%
Handling Instructions

TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).

For research use only. We do not sell to patients.

TAK-285 Chemical Structure

TAK-285 Chemical Structure

CAS No. : 871026-44-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 318 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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  • References

  • Customer Review

Description

TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity[1]. TAK-285 can cross the blood-brain barrier (BBB)[2].

IC50 & Target[1]

EGFR

23 nM (IC50)

HER2

17 nM (IC50)

In Vitro

TAK-285 (Compound 34e) shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM[1]. TAK-285 (Compound 34e) exhibits HER4 inhibitory activity with an IC50 value of 260 nM. TAK-285 also inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK and Lyn B with IC50s of 1100 nM, 5700 nM, 4200 nM, 1700 nM, 2400 nM, 4700 nM and 5200 nM, respectively[1].

In Vivo

TAK-285 (Compound 34e; 50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice[1].

Animal Model: Female BALB/cAJcl mice (7-weeks old) with 4−1ST xenograft models[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral administration; twice daily; for 14 days
Result: Exhibited dose-dependent tumor growth inhibition.
Clinical Trial
Molecular Weight

547.96

Formula

C₂₆H₂₅ClF₃N₅O₃

CAS No.

871026-44-7

SMILES

ClC(C=C(NC1=NC=NC2=C1N(CCNC(CC(C)(C)O)=O)C=C2)C=C3)=C3OC4=CC=CC(C(F)(F)F)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (91.25 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8250 mL 9.1248 mL 18.2495 mL
5 mM 0.3650 mL 1.8250 mL 3.6499 mL
10 mM 0.1825 mL 0.9125 mL 1.8250 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.16%

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Keywords:

TAK-285TAK285TAK 285EGFREpidermal growth factor receptorErbB-1HER1HER2orallyantitumorCNSpenetrationInhibitorinhibitorinhibit

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TAK-285
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HY-15196
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