Valecobulin hydrochloride

SKU: orb1308964

Description

Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of the vascular disrupting agent S516. It acts as a potent inhibitor of β-tubulin polymerization, demonstrating significant anti-tumor activity in preclinical models of solid tumors, including in vivo mouse studies and in vitro cytotoxicity assays.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1240321-53-2
• MW: 573.06
• Purity: 99.52% (May vary between batches)
• Formula: C₂₆H₂₉ClN₆O₅S
• SMILES: Cl.COc1cc(cc(OC)c1OC)C(=O)c1ccc(cc1-n1cncn1)-c1csc(NC(=O)[C@@H](N)C(C)C)n1
• Target: Microtubule Associated
• Solubility: DMSO:125 mg/mL (218.13 mM);H2O:50 mg/mL (87.25 mM)

Bioactivity

• In Vivo:
  METHODS: Nude mice carrying human colonic HCT116 and human colonic overexpression of the P-gp transporter HCT15 were treated with Valecobulin hydrochloride (CKD-516 hydrochloride) (5 mg/kg and 10 mg/kg, intraperitoneal injection, Q4D 4). RESULTS The IR of Valecobulin hydrochloride (CKD-516 hydrochloride) in HCT116 nude mice was 36% and 65%, respectively, and tumor growth was significantly inhibited in a dose-dependent manner; Valecobulin hydrochloride (CKD-516 hydrochloride) also showed resistance to MDR The potent antitumor activity of positive cell lines (HCT15), with IRs of 12% and 5%, respectively.
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Storage & Handling

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

Alternative Names

CKD 516, CKD 516 Hydrochloride, CKD516, CKD-516, CKD516 Hydrochloride, CKD-516 hydrochloride, CKD-516 Hydrochloride, antitumor, inhibit, MicrotubuleAssociated, Microtubule/Tubulin, Microtubule Associated, Inhibitor, prodrug, S516, β-tubulin polymerization, β-tubulin, Valecobulin, Valecobulin hydrochloride, Valecobulin Hydrochloride, VDA

Compound Identifiers

PubChem CID

46929961