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Camonsertib

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Catalog No. T62083Cas No. 2417489-10-0
Alias RP-3500, ATR inhibitor 4

Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.

Camonsertib

Camonsertib

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Purity: 99.93%
Catalog No. T62083Alias RP-3500, ATR inhibitor 4Cas No. 2417489-10-0
Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$172In StockIn Stock
5 mg$438In StockIn Stock
10 mg$637In StockIn Stock
25 mg$993In StockIn Stock
50 mg$1,320-In Stock
100 mg$1,820-In Stock
200 mg$2,450-In Stock
1 mL x 10 mM (in DMSO)$396In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.93%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.
Targets&IC50
ATR:1 nM, mTOR:120 nM
In vitro
METHODS: Characterization of the DNA damage response (DDR) to Camonsertib (RP-3500)-mediated ATR inhibition in LoVo and CW-2 human colon cancer cell lines treated with 1 μmol/L RP-3500 for varying durations up to 24 hours.
RESULTS Camonsertib (RP-3500) inhibits CHK1 (Ser345) phosphorylation 1-3 hours after initiation of treatment. [2]
METHODS: A biochemical assay for ATR/ATRIP inhibition was established using tagged human ATR and ATRIP purified from mammalian cells, with p53 (Ser15) as the phosphorylation substrate.
RESULTS In a LoVo cell-based assay, Camonsertib (RP-3500) inhibited gemcitabine-stimulated phosphorylation of the ATR substrate pCHK1 (Ser345) with an IC50 of 0.33 nM. [2]
In vivo
METHODS: Patients received Camonsertib (RP-3500) at doses ranging from 5-200 mg once daily or 40 to 80 mg twice daily for 5 days/2 days off (5/2) or 3 days/4 days off ( 3/4), hematological parameters were assessed over a range of doses during treatment.
RESULTS Early decrease in monocytes and reticulocytes on day 8 and further decrease in hemoglobin levels on day 15. [1]
METHODS: Camonsertib (RP-3500) was used to treat LoVo tumor xenografts in mice, orally administered once a day at a dose of 3/7/15 mg/kg for 17 days, and the effect on LoVo tumor xenografts in mice was observed.
RESULTS Camonsertib (RP-3500) treatment of LoVo tumor xenografts in mice produced dose-dependent tumor growth inhibition, with a minimum effective dose (MED) of 7 mg/kg. [2]
METHODS: In the CW-2 colon xenograft model, Camonsertib (RP-3500) was administered at doses of 5 and 10 mg/kg to observe the effects on the growth of the mouse CW-2 colon xenograft model.
RESULTS Treatment of xenograft mice with Camonsertib (RP-3500) produced statistically significant tumor growth inhibition. [2]
SynonymsRP-3500, ATR inhibitor 4
Chemical Properties
Molecular Weight410.47
FormulaC21H26N6O3
Cas No.2417489-10-0
SmilesC[C@@H]1COCCN1c1cc(c2cnn(-c3cc[nH]n3)c2n1)[C@@]1(O)C[C@@H]2CC[C@H](C1)O2
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (109.63 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1.5 mg/mL (3.65 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4362 mL12.1812 mL24.3623 mL121.8116 mL
5 mM0.4872 mL2.4362 mL4.8725 mL24.3623 mL
10 mM0.2436 mL1.2181 mL2.4362 mL12.1812 mL
20 mM0.1218 mL0.6091 mL1.2181 mL6.0906 mL
50 mM0.0487 mL0.2436 mL0.4872 mL2.4362 mL
100 mM0.0244 mL0.1218 mL0.2436 mL1.2181 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
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Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
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