TB22 inhibited the proliferation of H460R231Q cells with an IC50 value of 2.85 μM, about 13-fold more potent than SGC0946. Notably, TB22 demonstrated significant in vivo efficacy (TGI = 60.57%) in H460R231Q cell derived xenograft models and improved pharmacokinetic properties (t1/2 = 6.06 } 2.94 h and CL = 55.18 } 8.56 mL/kg/min). Moreover, a mechanism study validated that TB22 suppressed malignant phenotypes of lung cancer cells harboring R231Q mutation via the MAPK/ERK signaling pathway.
MedKoo Cat#: 127820
Name: TB-22
CAS#: N/A
Chemical Formula: C32H46ClN7O3S
Exact Mass: 643.3071
Molecular Weight: 644.28
Elemental Analysis: C, 59.66; H, 7.20; Cl, 5.50; N, 15.22; O, 7.45; S, 4.98
The following data is based on the product molecular weight 644.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
