IMR-1A
IMR-1A Basic information
- Product Name:
- IMR-1A
- Synonyms:
-
- IMR-1A
- IMR1A;IMR 1A;IMR-1A
- IMR-1A, >98%
- Acetic acid, 2-[2-methoxy-4-[(4-oxo-2-thioxo-5-thiazolidinylidene)methyl]phenoxy]-
- 2-(2-Methoxy-4-((4-oxo-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetic acid
- Notch,Inhibitor,inhibit,IMR1A,IMR-1A,IMR 1A,Drug Metabolite
- IMR-1A, 10 mM in DMSO
- IMR-1A ，S0225
- CAS:
- 331862-41-0
- MF:
- C13H11NO5S2
- MW:
- 325.36
- Mol File:
- 331862-41-0.mol
IMR-1A Chemical Properties
- Density
- 1.55±0.1 g/cm3(Predicted)
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- solubility
- DMSO:4.0(Max Conc. mg/mL);12.29(Max Conc. mM)
Water:1.0(Max Conc. mg/mL);3.07(Max Conc. mM) - pka
- 3.10±0.10(Predicted)
- form
- Solid
- color
- Light yellow to yellow
IMR-1A Usage And Synthesis
Uses
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A[1].
Biological Activity
IMR-1A is a potent inhibitor of Notch with IC50 of 0.5 μM and Kd of 2.9 μM. It has antitumor activity.
in vivo
IMR-1A (2 mg/kg (iv) and 100 mg/kg (ip)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/ 2) of 2.22 h following a single iv administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after ip administration.
| Animal Model: | Male C57 BL/6 mice |
| Dosage: | 2 mg/kg (iv) and 100 mg/kg (ip) |
| Iv and ip | |
| Result: | Exhibited low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single iv administration and plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after ip administration. |
target
| Target | Value |
| Notch (Cell-free assay) | 0.5 μM |
| Notch (Cell-free assay) | 2.9 μM(Kd) |