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Tarloxotinib bromide
🥰Excellent
Catalog No. T13088Cas No. 1636180-98-7
Alias TH-4000
Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.
Tarloxotinib bromide
🥰Excellent
Purity: 97.15%
Catalog No. T13088Alias TH-4000Cas No. 1636180-98-7
Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $143 | In Stock | |
| 5 mg | $297 | In Stock | |
| 10 mg | $455 | In Stock | |
| 25 mg | $745 | In Stock | |
| 50 mg | $987 | In Stock | |
| 100 mg | $1,380 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $459 | In Stock |
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Purity:97.15%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Smiles | [Br-].Cn1cnc(c1C[N+](C)(C)C\C=C\C(=O)Nc1cc2c(Nc3ccc(Cl)c(Br)c3)ncnc2cn1)[N+]([O-])=O |
| Relative Density. | 1.31g/cm3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 33 mg/mL (48.40 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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