2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. ATM/ATR mTOR
  4. Camonsertib

Camonsertib  (Synonyms: RP-3500; ATR inhibitor 4)

Cat. No.: HY-139609 Purity: 99.75%
COA Handling Instructions

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Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.

For research use only. We do not sell to patients.

Camonsertib Chemical Structure

Camonsertib Chemical Structure

CAS No. : 2417489-10-0

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1 mg USD 210 In-stock
5 mg USD 530 In-stock
10 mg USD 770 In-stock
25 mg USD 1200 In-stock
50 mg USD 1600 In-stock
100 mg USD 2200 In-stock
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Based on 1 publication(s) in Google Scholar

Camonsertib Related Antibodies

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Description

Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity[1].

IC50 & Target[1]

ATR

 

ATM

>30 μM (IC50)

mTOR

120 nM (IC50)

In Vitro

Camonsertib (RP-3500; 1 μM; 1-24 hours) inhibits CHK1(Ser345) phosphorylation from 1 to 3 hours[1].
Camonsertib inhibits Gemcitabine stimulated ATR phosphorylation of its substrate pCHK1(Ser345) with an IC50 of 0.33 nM in a LoVo cell-based assay[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Camonsertib Related Antibodies

Western Blot Analysis[1]

Cell Line: LoVo and CW-2 human colon cancer cell lines
Concentration: 1 μM
Incubation Time: 1, 2, 4, 6, 8, 16, 24 hours
Result: Inhibited CHK1(Ser345) phosphorylation from 1 to 3 hours. Starting at 4 hours, CHK1(Ser345) became re-phosphorylated as DNA-PKcs became activated in treated cells, along with its substrates KAP1 and H2AX.
In Vivo

Camonsertib (RP-3500; 3, 7, 15 mg/kg; Orally; once daily for 18 days) produces dose-dependent tumor growth inhibition with a minimum effective dose (MED) of 7 mg/kg in LoVo xenografts[1].
Camonsertib (5, 10 mg/kg; Orally; once daily) produces statistically significant tumor growth inhibition in the CW-2 colon xenograft model[1].
Camonsertib (7 mg/kg; for 7 days) results in 8.1- and 2.7-fold inductions of KAP1 and DNA-PKcs phosphorylation in mice bearing LoVo tumors[1].
Camonsertib has a more profound anti-tumor effect occurred at higher doses on the 3 days on/4 days off (30 mg/kg) and 5 days on/2 days off (25 mg/kg) schedules compared with consecutive daily administrations (10 mg/kg) at a lower dose for 14 days[1].
Camonsertib (15mg/kg) combined PARPi Olaparib (80mg/kg; both agents days 1-3 on/4 days off) or sequential (PARPi for 3 days followed by RP-3500 for 3 days then 1 day off) schedules produces greater antiTumor effects compared with sequential administration without affecting tolerability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female mice (6-8 weeks old) bearing LoVo xenografts[1]
Dosage: 3, 7, 15 mg/kg (0.5% methylcellulose/0.02% SDS vehicle)
Administration: Orally; once daily for 18 days
Result: Produced dose-dependent tumor growth inhibition with a minimum effective dose (MED) of 7 mg/kg.
The maximum tolerated dose (MTD) was 10 mg/kg once daily on a continuous dosing schedule.
Clinical Trial
Molecular Weight

410.47

Formula

C21H26N6O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@]1(C[C@H]2O[C@H](CC2)C1)C3=C4C(N(C5=NNC=C5)N=C4)=NC(N6[C@@H](COCC6)C)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (121.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4362 mL 12.1812 mL 24.3623 mL
5 mM 0.4872 mL 2.4362 mL 4.8725 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.75%

COA (260 KB) HNMR (212 KB) RP-HPLC (259 KB) LCMS (153 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4362 mL 12.1812 mL 24.3623 mL 60.9058 mL
5 mM 0.4872 mL 2.4362 mL 4.8725 mL 12.1812 mL
10 mM 0.2436 mL 1.2181 mL 2.4362 mL 6.0906 mL
15 mM 0.1624 mL 0.8121 mL 1.6242 mL 4.0604 mL
20 mM 0.1218 mL 0.6091 mL 1.2181 mL 3.0453 mL
25 mM 0.0974 mL 0.4872 mL 0.9745 mL 2.4362 mL
30 mM 0.0812 mL 0.4060 mL 0.8121 mL 2.0302 mL
40 mM 0.0609 mL 0.3045 mL 0.6091 mL 1.5226 mL
50 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.2181 mL
60 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0151 mL
80 mM 0.0305 mL 0.1523 mL 0.3045 mL 0.7613 mL
100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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Camonsertib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Camonsertib2417489-10-0RP-3500 ATR inhibitor 4RP3500RP 3500ATR inhibitor4ATR inhibitor 4ATR inhibitor-4ATM/ATRmTORAtaxia telangiectasia mutatedATM and RAD3 relatedMammalian target of RapamycinorallyATRiDNA-PKCHK1(Ser345) phosphorylationLoVoCW-2Inhibitorinhibitorinhibit

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