A Smac mimetic and inhibitor of IAP family proteins
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LCL-161

Item No. 22420

Technical Information
Formal Name
N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2S-(methylamino)-propanamide
CAS Number
1005342-46-0
Synonyms
  • NVP-LCL161
Molecular Formula
C26H33FN4O3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/ml
λmax
271 nm
SMILES
O=C(N1CCC[C@H]1C2=NC(C(C3=CC=C(F)C=C3)=O)=CS2)[C@@H](NC([C@@H](NC)C)=O)C4CCCCC4
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
InChi Key
UFPFGVNKHCLJJO-SSKFGXFMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LCL-161 is a small molecule Smac mimetic that inhibits multiple inhibitor of apoptosis (IAP) family proteins.1 As a single agent, LCL-161 inhibits growth of FLT3-ITD-expressing leukemia cells via induction of apoptosis with IC50 values ranging from 0.5-4 μM. In vivo, LCL-161 enhances growth inhibition driven by PKC 412 (Item No. 10459) in a mouse Ba/F3-FLT3-ITD-luc+ leukemia xenograft model. It exhibits additive effects with the chemotherapeutic agents doxorubicin (Item No. 15007) and cytarabine (Item No. 16069). LCL-161 also inhibits growth of nilotinib-resistant leukemia cell lines and exhibits synergy with nilotinib (Item No. 10010422) in a Bcr-Abl expressing, 32D.p20-luc+ leukemia mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Weisberg, E., Ray, A., Barrett, R., et alSmac mimetics: Implications for enhancement of targeted therapies in leukemia. Leukemia 24(12), 2100-2109 (2010).