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Tarloxotinib bromide
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Tarloxotinib bromide
Catalog No. T13088Cas No. 1636180-98-7
Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $175 | In Stock | |
| 5 mg | $372 | In Stock | |
| 10 mg | $556 | In Stock | |
| 25 mg | $896 | In Stock | |
| 50 mg | $1,220 | In Stock | |
| 100 mg | $1,650 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $559 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2. |
| In vitro | Tarloxotinib bromide is 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[1]. |
| In vivo | Tarloxotinib bromide treatment regresses the WT EGFR NSCLC tumor models H125 and H1648, demonstrating Tarloxotinib bromide provides the necessary therapeutic index to inhibit WT EGFR in vivo[2]. |
| Alias | TH-4000 |
| Molecular Weight | 681.77 |
| Formula | C24H24Br2ClN9O3 |
| Cas No. | 1636180-98-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||
| Solubility Information | DMSO: 33 mg/mL (48.40 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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