RP-6306

SKU: orb1689144

Description

Lunresertib (RP-6306) is an orally bioavailable, selective PKMYT1 inhibitor with 14 nM potency. It demonstrates robust antitumor activity in preclinical models, particularly against CCNE1-amplified cancers, supporting its investigation in oncology research for targeted therapeutic strategies.

Research Area

Cell Biology

Key Properties

• CAS Number: 2719793-90-3
• MW: 324.38
• Purity: 99.80% (May vary between batches)
• Formula: C₁₈H₂₀N₄O₂
• SMILES: NC=1N(C=2C(C1C(N)=O)=CC(C)=C(C)N2)C3=C(C)C(O)=CC=C3C
• Target: Wee1
• Solubility: DMSO:67.3 mg/mL (207.47 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.17 mM)

Bioactivity

• Target IC50:
  CDK1-pY15 cells:> 2 μM|CDK1-pT14 cells:7.5 ± 1.8 nM|PKMYT1:14 nM
• In Vivo:
  METHODS: lunresertib (RP-6306) (3, 10 and 60 mg/kg, oral, daily) was used to treat CCNE1-amplified ovary xenograft model (OVCAR3) mice, and tumor growth in the mice was observed. RESULTS lunresertib (RP-6306) inhibited tumor growth in OVCAR3 mice in a statistically significant concentration-dependent manner.
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• In Vitro:
  METHODS: HCC1569 breast cancer cell line was treated with lunresertib (RP-6306) (63, 125, 250, 500 nM) to assess whether PKMYT1 inhibition leads to DNA damage in CCNE1-high cells by monitoring γH2AX levels using quantitative image-based flow cytometry. RESULTS Treatment with lunresertib (RP-6306) induced pan-γH2AX in the HCC1569 breast cancer cell line, suggesting that tumor-derived CCNE1 amplification also renders cells susceptible to DNA damage induction following PKMYT1 inhibition.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

(S)-RP-6306, RP 6306, RP6306, RP-6306, PKMYT1

Compound Identifiers

PubChem CID

156869388