YX-2-107

SKU: orb1982695

Description

YX-2-107 is a potent and selective CDK6-targeting PROTAC degrader (IC50 = 4.4 nM). It demonstrates efficacy in vitro by suppressing RB phosphorylation and FOXM1, and inhibits Ph+ ALL progression in rat models, supporting its research application for this leukemia type.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2417408-46-7
• MW: 889.95
• Purity: 98.09% (May vary between batches)
• Formula: C₄₅H₅₁N₁₁O₉
• SMILES: O=C1NC(=O)C(N2C(=O)C=3C=CC=C(OCC(=O)NCCCCNCC(=O)N4CCN(C5=CN=C(C=C5)NC=6N=CC7=C(N6)N(C(=O)C(C(=O)C)=C7C)C8CCCC8)CC4)C3C2=O)CC1
• Target: PROTACs,CDK
• Solubility: DMSO:2.4 mg/mL (2.7 mM)

Bioactivity

• Target IC50:
  CDK6:4.4 nM
• In Vivo:
  Following a single intraperitoneal administration at a dose of 10 mg/kg, YX-2-107 achieves a maximum concentration of 741 nM in plasma after 4 hours. This concentration is 150-fold greater than the CDK6 degradation IC50. Clearance from the plasma is observed within the mentioned timeframe. Moreover, when administered at a dose of 150 mg/kg intraperitoneally, once daily for 3 days, YX-2-107 is pharmacologically active in suppressing the proliferation of Ph+ ALL in mice.
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• In Vitro:
  In Ph+ BV173 and SUP-B15 cells, YX-2-107, when applied at a concentration of 2000 nM for 48 hours, demonstrates inhibition of the S phase. Furthermore, at various concentrations (0, 1.6, 8, 40, 200, 1000 nM) for 4 hours, YX-2-107 selectively degrades CDK6 in BV173 cells. Additionally, when used at a concentration of 2000 nM for 72 hours, YX-2-107 inhibits RB phosphorylation and FOXM1 expression in Ph+ BV173 and SUP-B15 cells.
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Storage & Handling

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

Alternative Names

CDK6

Compound Identifiers

PubChem CID

166642460