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

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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

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Hazard and Precautionary Statements (GHS)

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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

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2417489-10-0, camonsertibRelated Search:

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)-

RP-3500

RP-3500 (Synonyms: ATR inhibitor 4)

camonsertib

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

Camonsertib, 10 mM in DMSO

Camonsertib (RP-3500)

2417489-10-0