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RP-6306 (Lunresertib) is the first-in-class, highly potent and selective PKMYT1 inhibitor that preferentially kills tumor cells overexpressing CCNE1 and was shown to inhibit the growth of a broad range of CCNE1-amplified tumors in xenograft/PDX preclinical models, both as a single agent and in combination therapy settings. RP-6306 inhibition of Thr14 phosphorylation of CDK1 in HCC1569.
In vivo, RP-6306 (15, 50, and 300 ppm; oral; daily; for 21 days) results in a statistically significant and dose-dependent reduction in OVCAR3 tumor growth in CCNE1-amplified ovarian xenograft model (OVCAR3).
| Molecular Weight | 324.38 |
| Formula | C18H20N4O2 |
| CAS Number | 2719793-90-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Wee1 Products |
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| WEE1-IN-5
WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. |
| WEE1-IN-4
WEE1-IN-4 is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM. |
| Pomalidomide-C3-adavosertib
Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis. |
| PD0166285 dihydrochloride
PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1. |
| ZN-c3
ZN-c3 is a potentially first-in-class and best-in-class orally active, potent and selective Wee1 inhibitor (IC50=3.9 nM). zN-c3 can be used in cancer research. |
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