RSH-7

SKU: orb2900550

Description

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

Research Area

Neuroscience

Key Properties

• CAS Number: 2764609-97-2
• MW: 436.49
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₅FN₈O
• SMILES: N(C1=C(C(NN)=O)C=CC=C1)C2=NC(NC3=CC=C(C=C3)N4CCN(C)CC4)=NC=C2F
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 83.33 mg/mL (190.91 mM; Ultrasonic )

Bioactivity

• In Vivo:
  RSH-7 (25, 50 mg/kg; i.p.; daily for 16 days) shows anti-tumor activity with significantly and dose-dependently suppresses the tumor growth in mouse. Animal model: Female NOD/SCID mice (jeko-1 cell-inoculated xenograft NOD/SCID mice models). Dosage: 25, 50 mg/kg. Administration: i.p.; daily for 16 days. Result: Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 66.95% and 79.78% at doses of 25 and 50 mg/kg,. Animal model: Female NOD/SCID mice (MV4-11 cell-inoculated xenograft NOD/SCID mice models). Dosage: 10, 20 mg/kg. Administration: i.p.; daily for 21 days. Result: Significantly and dose-dependently suppressed the tumor growth with the TGI rates of 74.23% and 94.84% at the dosage of 10 and 20 mg/kg, respectively.
  Read more...
• In Vitro:
  RSH-7 (1-1000 nM; 72 h) shows antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively. RSH-7 (30, 150, 750 nM; 72 h) decreases the expression of p-BTK (TYR223), p-PLCγ(Tyr1217), p-FLT3 (Tyr589), p-STAT5 (TYR694) in a dose-dependent manner. RSH-7 (30, 150, 750 nM; 72 h) induces apoptosis and increases the expression of BAX, p53, cleaved caspase 3 in a dose dependen manner in jeko-1 cells.. Cell Viability Assay Cell line: Jeko-1, MV-4-11, Molt4, K562 cells. Concentration: 1-1000 nM. Incubation time: 72 h. Result: Showed antiproliferative activities with IC50s of 17, 3, 11, 930 nM for Jeko-1, MV-4-11, Molt4, K562 cells, respectively. Western blot analysis. Cell line: jeko-1 cells. Concentration: 30, 150, 750 nM. Incubation time: 72 h. Result: Reduced both BTK, PLCγ2, FLT3 and STAT5 phosphorylation in a dose-dependent manner. Apoptosis Analysis Cell line: jeko-1 cells. Concentration: 30, 150, 750 nM. Incubation time: 72 h. Result: Dose-dependently induced cell apoptosis and upregulated the expression of pro-apoptotic protein BAX, p53, cleaved caspase 3.
  Read more...

Storage & Handling

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

Quick Database Links

Gene Symbol

Apoptosis