A Smac mimetic and inhibitor of IAP family proteins; inhibits growth of FLT3-ITD-expressing leukemia cells via induction of apoptosis (IC50s = 0.5-4 μM); enhances growth inhibition driven by PKC 412 in a mouse Ba/F3-FLT3-ITD-luc+ leukemia xenograft model; exhibits additive effects with the chemotherapeutic agents doxorubicin and cytarabine; inhibits growth of nilotinib-resistant leukemia cell lines and exhibits synergy with nilotinib in a Bcr-Abl expressing

LCL-161 – 10 mg

Brand:
Cayman
CAS:
1005342-46-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

LCL-161 is a small molecule Smac mimetic that inhibits multiple inhibitor of apoptosis (IAP) family proteins.{37162} 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.  

 

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Description

A Smac mimetic and inhibitor of IAP family proteins; inhibits growth of FLT3-ITD-expressing leukemia cells via induction of apoptosis (IC50s = 0.5-4 μM); enhances growth inhibition driven by PKC 412 in a mouse Ba/F3-FLT3-ITD-luc+ leukemia xenograft model; exhibits additive effects with the chemotherapeutic agents doxorubicin and cytarabine; inhibits growth of nilotinib-resistant leukemia cell lines and exhibits synergy with nilotinib in a Bcr-Abl expressing, 32D.p20-luc+ leukemia mouse xenograft model

Formal name: N-[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(4-fluorobenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]-2S-(methylamino)-propanamide

Synonyms:  NVP-LCL161

Molecular weight: 500.6

CAS: 1005342-46-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Multidrug Resistance

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