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Pyrotinib dimaleate
🥰Excellent
Catalog No. T12594Cas No. 1397922-61-0
Alias SHR-1258 dimaleate
Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.
Pyrotinib dimaleate
🥰Excellent
Purity: 99.52%
Catalog No. T12594Alias SHR-1258 dimaleateCas No. 1397922-61-0
Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $157 | In Stock | |
| 5 mg | $482 | In Stock | |
| 10 mg | $642 | In Stock | |
| 25 mg | $996 | In Stock | |
| 50 mg | $1,370 | In Stock | |
| 100 mg | $1,850 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $652 | In Stock |
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Purity:99.52%
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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 | Pyrotinib dimaleate is a selective EGFR/HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer. |
| Targets&IC50 | HER2:38 nM, EGFR:13 nM |
| In vitro | METHODS: SK-BR-3 cells were treated with Pyrotinib dimaleate (10nM) + chrysin (20μM) or drug + mimics and drug + si-ZBTB16, and the cells were collected for apoptosis analysis. RESULTS Pyrotinib dimaleate + chrysin treatment led to a significant upregulation of ZBTB16 expression, and this effect was neutralized by knockdown of ZBTB16 by siRNA-ZBTB16; miR-16-5p overexpression or ZBTB16 knockdown correspondingly reduced the apoptosis rate induced by Pyrotinib dimaleate + chrysin treatment. [2] |
| In vivo | METHODS: Nude mice with tumor xenografts of BT-474 or SK-BR-3 cells were treated with Pyrotinib dimaleate (10 mg/kg, gavage, 21 days), chrysin (50 mg/kg), or their combination, and the effect of miR-16-5p expression level on anti-tumor efficacy was analyzed. RESULTS Combination therapy of pyrotinib dimaleate and chrysin synergistically enhanced autophagy in HER2-positive breast cancer cells by regulating the miR-16-5p/ZBTB16/G6PD axis.[2] |
| Alias | SHR-1258 dimaleate |
| Molecular Weight | 815.22 |
| Formula | C40H39ClN6O11 |
| Cas No. | 1397922-61-0 |
| Smiles | OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)\C=C\[C@H]1CCCN1C |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 50 mg/mL (61.33 mM) Ethanol: 40 mg/mL (49.07 mM) DMSO: 100 mg/mL (122.67 mM) | |||||||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||||||||||||
Ethanol/H2O/DMSO
H2O/DMSO
DMSO
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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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