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Gartisertib
🥰Excellent
Catalog No. T10407Cas No. 1613191-99-3
Alias VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
Gartisertib
🥰Excellent
Catalog No. T10407Alias VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2Cas No. 1613191-99-3
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $136 | In Stock | |
| 5 mg | $338 | In Stock | |
| 10 mg | $565 | In Stock | |
| 25 mg | $1,130 | In Stock | |
| 50 mg | $1,570 | In Stock | |
| 100 mg | $2,360 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $403 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors. |
| Targets&IC50 | ATR:8 nM |
| In vitro | Gartisertib was four times more potent in all glioblastoma cell lines than the widely used ATR inhibitor berzosertib (Gartisertib median IC50 = 0.56 μM, berzosertib median IC50 = 2.21 μM). In addition, Gartisertib observed a higher IC50 (7.22 μM) in human astrocytes, indicating a lower potential toxicity of Gartisertib to normal brain cells. The combination of Gartisertib (1 μM) with TMZ+RT significantly increased apoptosis and cell death in patient-derived glioblastoma cell lines. [1] |
| In vivo | Gartisertib (10 mg/kg or 20 mg/kg) plus cisplatin inhibited tumor growth in metastatic clear cell renal cell carcinoma (ccRCC) xenografts, demonstrating therapeutic synergies. [2] |
| Alias | VX-803, VX 03, VRT1228692, M4344, M 4344, ATR inhibitor 2 |
| Molecular Weight | 541.55 |
| Formula | C25H29F2N9O3 |
| Cas No. | 1613191-99-3 |
| Smiles | O=C(NC=1C=NC=C(F)C1N2CCC(C(=O)N3CCN(CC3)C4COC4)CC2)C=5C(=NN6C=C(F)C=NC56)N |
| 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: 16 mg/mL (29.54 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
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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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