product name LCL161
References: Biochem Pharmacol. 2012 Aug 1;84(3):268-77; Pediatr Blood Cancer. 2012 Apr;58(4):636-9.
500.63
Formula
C26H33FN4O3S
CAS No.
1005342-46-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: Soluble in DMSO > 10 mM
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 20 mg/mL warming (39.94 mM)
Solubility (In vivo)
Chemical Name
(2S)-N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]-2-(methylamino)propanamide
other peoduct :
| LCL161 binds to inhibitors of apoptosis proteins (IAPs) with high affinity and initiates the destruction of cIAP1 and cIAP2, which further induces apoptosis via caspase activation. LCL161 modestly inhibits the growth of FLT3-ITD-expressing cells when administered alone, with an IC50 ranging from ~0.5 μM (Ba/F3-FLT3-ITD cells) to ~4 μM (MOLM13-luc+ cells). | |
|---|---|
| In Vivo | LCL161 significantly enhances the ability of PKC412 to inhibit the growth of Ba/F3-FLT3-ITD-luc+ cells in vivo. LCL161 is also shown to positively combine with the standard chemotherapeutic agents, Ara-c and doxorubicin, against FLT3-ITD-expressing cells and against D835Y-expressing cells. |
| Animal model | Huh-7 xeonograft nude mice |
| Formulation & Dosage | 50 mg/kg; p.o.; q.d., for 20 days |
| References | Biochemical pharmacology, 2012, 84(3): 268-277. |
