camonsertib
- Product Name
- camonsertib
- CAS No.
- 2417489-10-0
- Chemical Name
- camonsertib
- Synonyms
- RP-3500;camonsertib;ATR inhibitor 4;Camonsertib (RP-3500);Camonsertib, 10 mM in DMSO;RP-3500 (Synonyms: ATR inhibitor 4);(3-endo)-3-(6-((R)-3-Methylmorpholino)-1-(1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl)-8-oxabicyclo[3.2.1]octan-3-ol;(1R,5S)-3-{6-[(3R)-3-methylmorpholin-4-yl]-1-(1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl}-8-oxabicyclo[3.2.1]octan-3-ol;8-Oxabicyclo[3.2.1]octan-3-ol, 3-[6-[(3R)-3-methyl-4-morpholinyl]-1-(1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridin-4-yl]-, (3-endo)-
- CBNumber
- CB19804936
- Molecular Formula
- C21H26N6O3
- Formula Weight
- 410.48
- MOL File
- 2417489-10-0.mol
camonsertib Property
- Boiling point:
- 666.8±55.0 °C(Predicted)
- Density
- 1.61±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- form
- Solid
- pka
- 10.79±0.10(Predicted)
- color
- White to off-white
- InChIKey
- YIHHYCIYAIVQKX-UHFFFAOYSA-N
- SMILES
- OC1(CC2CCC(O2)C1)C1C=C(N2CCOCC2C)N=C2N(C3=NNC=C3)N=CC=12
camonsertib Chemical Properties,Usage,Production
Uses
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].
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].
| 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. |
IC 50
ATR; ATM: >30 μM (IC50); mTOR: 120 nM (IC50)
References
[1] Anne Roulston, et al. RP-3500: A Novel, Potent and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors. Mol Cancer Ther DOI:10.1158/1535-7163.MCT-21-0615
camonsertib Preparation Products And Raw materials
Raw materials
Preparation Products
camonsertib Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
- 58
- Tel
- tp@aladdinsci.com
- Country
- United States
- ProdList
- 52923
- Advantage
- 58