1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Tarloxotinib bromide

Tarloxotinib bromide (Synonyms: TH-4000)

Cat. No.: HY-17632 Purity: 98.97%
Handling Instructions

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.

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

Tarloxotinib bromide Chemical Structure

Tarloxotinib bromide Chemical Structure

CAS No. : 1636180-98-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 675 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.

IC50 & Target[1]

EGFR/HER2

 

In Vitro

To confirm the mechanism of action, Tarloxotinib bromide is shown to be metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release <0.002 nM/hr/106 cells). Cellular anti-proliferative and receptor phosphorylation assays demonstrate a 14-80 fold reduction of Tarloxotinib bromide activity relative to TKI. Using PC9 tumors, hyperbaric oxygen breathing suppresse release of TKI from Tarloxotinib bromide by >80% (538 vs 99 nM/kg; p<0.01) compared to air breathing controls. Collectively, these data further validate that Tarloxotinib bromide is a hypoxia-activated irreversible EGFR-TKI, and show that Tarloxotinib bromide has greater activity compared with erlotinib[2].

In Vivo

A prototypic WT EGFR driven xenograft model (A431) is used to benchmark Tarloxotinib bromide activity against each EGFR-TKI by “retrotranslation” of reported plasma exposure for each agent in human subjects back to the xenograft model. Only treatment with clinically relevant doses and schedules of Tarloxotinib bromide is associated with tumor regression and durable inhibition of WT EGFR tumor phosphorylation. Consistent with these findings, Tarloxotinib bromide treatment can also regress the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo[1].

Clinical Trial
Molecular Weight

681.77

Formula

C₂₄H₂₄Br₂ClN₉O₃

CAS No.

1636180-98-7

SMILES

BrC1=C(Cl)C=CC(NC2=NC=NC3=C2C=C(NC(/C=C/C[N+](C)(C)CC4=C([N+]([O-])=O)N=CN4C)=O)N=C3)=C1.[Br-]

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 : ≥ 33 mg/mL (48.40 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4668 mL 7.3339 mL 14.6677 mL
5 mM 0.2934 mL 1.4668 mL 2.9335 mL
10 mM 0.1467 mL 0.7334 mL 1.4668 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (3.67 mM); Clear solution

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

TarloxotinibTH-4000TH4000TH 4000EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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Product name:
Tarloxotinib bromide
Cat. No.:
HY-17632
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