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Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $228 | In Stock | |
50 mg | $378 | In Stock | |
100 mg | $591 | In Stock | |
500 mg | $1,270 | In Stock | |
1 mL x 10 mM (in DMSO) | $79 | In Stock |
Description | Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride. |
Targets&IC50 | ATR:7 nM (IC50) |
In vivo | The novel selective ATR kinase inhibitor Elimusertib on tumor cell growth and viability.Potent antiproliferative activity was demonstrated in a broad spectrum of human tumor cell lines.Elimusertib exhibited strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.The combination of Elimusertib with DNA damage-inducing chemotherapy or external beam radiotherapy (EBRT) showed synergistic antitumor activity.Combination treatment with Elimusertib and DDR inhibitors achieved strong synergistic antiproliferative activity in vitro, and combined inhibition of ATR and PARP signaling using olaparib demonstrated synergistic antitumor activity in vivo Furthermore, the combination of Elimusertib with the novel, nonsteroidal androgen receptor antagonist darolutamide resulted in significantly improved antitumor efficacy compared with respective single-agent treatments in hormone-dependent prostate cancer,and addition of EBRT resulted in even further enhanced antitumor efficacy[1]. |
Alias | BAY-1895344 |
Molecular Weight | 375.43 |
Formula | C20H21N7O |
Cas No. | 1876467-74-1 |
Smiles | C[C@@H]1COCCN1c1cc(-c2ccnn2C)c2ccnc(-c3cc[nH]n3)c2n1 |
Relative Density. | 1.43 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 11 mg/mL (29.3 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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