XMD8-87

SKU: orb1226710

Description

XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM; completely inhibits A549 cancer cell growth, and partially inhibited EGF-stimulated cancer cell growth at 10 uM; XMD8-87 is a potent, selective Ack1 (TNK2) inhibitor with IC50 of 1.9 uM in ELISA assays; potently block proliferation of TNK2 mutant cell lines, shows IC50s of 38 nM and 113 nM for the D163E and R806Q mutations.(In Vitro):XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87.

Key Properties

• CAS Number: 1234480-46-6
• MW: 445.527
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₇N₇O₂
• SMILES: C1=NC(NC2=CC=C(N3CCN(C)CC3)C=C2OC)=NC2N(C)C3C=CC=CC=3C(=O)NC1=2
• Target: Ack1 (TNK2)
• Solubility: DMSO: 65 mg/mL (145.89 mM)Ethanol: 5 mg/mL (11.2 mM)Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1, 000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ack1 inhibitor B19

Quick Database Links

Gene Symbol

Ack1 (TNK2)