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

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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5 mg USD 640 In-stock
10 mg USD 1020 In-stock
25 mg USD 2020 In-stock
50 mg USD 3200 In-stock
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Based on 1 publication(s) in Google Scholar

Camonsertib Related Antibodies

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  • Biological Activity

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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].

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].

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

Appearance

Solid

Formula

C21H26N6O3
CAS No.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.75%

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

Handling Instructions (2659 KB)
References
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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.

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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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