| CAS NO: | 1005342-46-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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) | |
| Other info | Synonym: LCL161; LCL 161; LCL-161 Chemical Name: (S)-N-((S)-1-cyclohexyl-2-((S)-2-(4-(4-fluorobenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)-2-(methylamino)propanamide InChi Key: UFPFGVNKHCLJJO-SSKFGXFMSA-N InChi Code: InChI=1S/C26H33FN4O3S/c1-16(28-2)24(33)30-22(17-7-4-3-5-8-17)26(34)31-14-6-9-21(31)25-29-20(15-35-25)23(32)18-10-12-19(27)13-11-18/h10-13,15-17,21-22,28H,3-9,14H2,1-2H3,(H,30,33)/t16-,21-,22-/m0/s1 SMILES Code: C[C@H](NC)C(N[C@@H](C1CCCCC1)C(N2[C@H](C3=NC(C(C4=CC=C(F)C=C4)=O)=CS3)CCC2)=O)=O |
| 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 |
| In Vitro | 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. |
 Weisberg E, et al. Leukemia, 2010, 24(12), 2100-2109. |  Effects of IAP inhibitor treatment and FLT3 inhibition, alone and combined, on the growth of mutant FLT3-expressing cells in vivo |  Effects of IAP inhibitor treatment and Abl inhibition, alone and combined, on the growth of BCR-ABL-expressing cells in vitro and in vivo |
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