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Camonsertib
🥰Excellent
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
🥰Excellent
Purity: 99.6%
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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $172 | In Stock | |
| 5 mg | $438 | In Stock | |
| 10 mg | $637 | In Stock | |
| 25 mg | $993 | In Stock | |
| 50 mg | $1,320 | In Stock | |
| 100 mg | $1,820 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $495 | In Stock |
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Purity:99.6%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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 kinase: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] |
| Alias | RP-3500, ATR inhibitor 4 |
| Molecular Weight | 410.47 |
| Formula | C21H26N6O3 |
| Cas No. | 2417489-10-0 |
| Smiles | C[C@@H]1COCCN1c1cc(c2cnn(-c3cc[nH]n3)c2n1)[C@@]1(O)C[C@@H]2CC[C@H](C1)O2 |
Storage & Solubility Information
| Storage | store at low temperature,keep away from direct sunlight | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45.0 mg/mL (109.6 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
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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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