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

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

製品番号: HY-139609 純度: 99.99%
COA 取扱説明書 Technical Support

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.

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Camonsertib

Camonsertib 構造式

CAS 番号 : 2417489-10-0

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 583 在庫あり
Solution
10 mM * 1 mL in DMSO USD 583 在庫あり
Solid
1 mg $210 在庫あり
5 mg $530 在庫あり
10 mg $770 在庫あり
25 mg $1200 在庫あり
50 mg $1600 在庫あり
100 mg $2200 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Camonsertib 関連抗体

Top Publications Citing Use of Products

ATM/ATR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
ATM ATR TRRAP

mTOR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mTOR mTORC1 mTORC2

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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)

Cellular Effect
Cell Line Type Value Description References
LoVo IC50
28 nM
Compound: 30; RP-3500
Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay
Cytotoxicity against human LoVo cells assessed as reduction in cell viability incubated for 5 days by CellTiter-Glo assay
[PMID: 38299539]
体外実験

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 関連抗体

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.
体内実験

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.
臨床実験
分子量

410.47

分子式

C21H26N6O3
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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)
溶剤 & 溶解度
体外: 

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
10 mM 0.2436 mL 1.2181 mL 2.4362 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

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C2

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体内:

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

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(per animal)

g

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(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.
純度とドキュメンテーション

純度: 99.99%

COA (260 KB) HNMR (191 KB) RP-HPLC (320 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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