LFM-A13

SKU: orb1225538

Description

A highly specific inhibitor of BTK with Ki of 1.4 uM, IC50 of 17.2 uM; shows no activity against EGFR, IRK, JAK1, JAK3, or HCK; enhances the sensitivity to ceramide- or vincristine-induced apoptosis in BTK+ B-lineage leukemic cells; prolongs the median survival time of VPL-treated mice; also inhibits Plk3 with IC50 of 61 uM, prevented bipolar mitotic spindle assembly in human breast cancer cells and glioblastoma cells, delays tumor progression in MMTV/neu transgenic mouse model of HER2 positive breast cancer.

Key Properties

• CAS Number: 244240-24-2
• MW: 360.0014
• Purity: >98% (HPLC)
• Formula: C₁₁H₈Br₂N₂O₂
• SMILES: C/C(O)=C(C#N)/C(NC1=CC(Br)=CC=C1Br)=O
• Target: BTK
• Solubility: DMSO: ≥ 42 mg/mL

Bioactivity

• In Vivo:
  LFM-A13 (25, 50 and 100 mg/kg) shows no apparent toxicity to rats. LFM-A13 (50 mg/kg, three times a week, i.p.) attenuatesmammary tumorigenesis in mice. LFM-A13 alone or in combination with paclitaxel shows marked effect on the breast tumor incidence, mean tumor numbers, average tumor weight, and size in BALB/c mice. LFM-A13 (50 mg/kg, three times a week, i.p.) significantly decreases PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increases the expression of p21, IκB, Bax and caspase 3 expression in mice. LFM-A13 (200 mg/kg) does not cause hematologic toxicity in rats. LFM-A13 (10 or 50 mg/kg, i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer.
• In Vitro:
  LFM-A13 significantly inhibits BTK activity with an IC50 of 6.2 ± 0.3 μg/mL (= 17.2 ± 0.8 μM). The calculated Kis of LFM-A13 for BTK, JAK1, JAK3, IRK, EGFR and HCK are 1.4, 110, 148, 31.6, 166 and 214 μM. LFM-A13 (200 μM) markedly increases the chemosensitivity of ALL-1 cells to ceramide-induced apoptosis. LFM-A13 (100 μM) suppresses Epo-induced phosphorylation of EpoR, Jak2, Btk, Stat5 and Erk1/2 in R10 cells. LFM-A13 (100 μM) inhibits auto-phosphorylation of Jak2, Tec and Btk rather than Lyn kinase auto-phosphorylation in COS cells. LFM-A13 potently inhibits Plx1 with IC50 of 10 μM; also inhibits BRK, BMX, FYN and with IC50s of 267, 281, 240 and 215 μM.

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

LFM A13 | LFM-A13 | LFM A13

Quick Database Links

Gene Symbol

BTK