Lunresertib free base · Synonyms: RP-6306 | (S)-RP-6306 | (S)-RP-6306 (compound 181)
RP-6306 is a Protein Kinase, Membrane Associated Tyrosine/Threonine 1 inhibitor.
For research use only. Not for human or veterinary use.
Description
RP-6306 is a Protein Kinase, Membrane Associated Tyrosine/Threonine 1 (PKMYT1) inhibitor, which can be used for the research of cancer.
Biological activity
In Vitro lunresertib (500 nM; for 24 h) treatment induces pan-γH2AX in an HCC1569 breast cancer cell line, indicating that tumour-derived CCNE1 amplification also renders cells vulnerable to DNA damage induction following PKMYT1 inhibition. lunresertib treatment causes unscheduled activation of CDK1 selectively in CCNE1-overexpressing cells, promoting early mitosis in cells undergoing DNA synthesis. In Vivo lunresertib (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).
Identifiers
- SMILES
-
O=C(N)C=1C=2C=C(C(=NC2N(C1N)C=3C(=CC=C(O)C3C)C)C)C - InChIKey
-
ARBRHWRTXPWZGN-UHFFFAOYSA-N
Specifications
- MW (average)
- 324.3770
- Formula
- C18H20N4O2
- CAS No.
- 2719793-90-3
- Physical state
- Solid
- Color
- Off-white to gray
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO 50 mg/mL
Documents
References
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