BiochemProbe — Life Science Research Reagents

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.

Target Wee1
Research area Cancer
Purity HPLC >98%; SFC >98%; Stock Inquire

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

References

[1]. Szychowski J, et al. Compounds, pharmaceutical compositions, and methods of preparing compounds and their use. WO2021195781A1.
[2]. David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(7907):749-756.

Same target

Search Wee1

Same research area

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