Cat.NO.:A188719 Purity:98%
Product Details of LCL161
| CAS No. : | 1005342-46-0 |
| Formula : |
C26H33FN4O3S |
| M.W : |
500.63
|
| 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 |
| Synonyms : |
NVP-LCL161
|
| MDL No. : | MFCD23160049 |
| InChI Key : | UFPFGVNKHCLJJO-SSKFGXFMSA-N |
| Pubchem ID : | 24737642 |
Safety of LCL161
| GHS Pictogram: |  |
| Signal Word: | Warning |
| Hazard Statements: | H302 |
| Precautionary Statements: | P280-P305+P351+P338 |
Isoform Comparison
Biological Activity
| Target |
|
In Vitro:
| Concentration | Treated Time | Description | References |
| A549 | 0–200μM | 48 hours | To evaluate the cytotoxic effects of LCL161 and paclitaxel, results showed that paclitaxel significantly reduced cell viability, while LCL161 alone had minimal effect. | PMC5062899 |
| H460 | 0–200μM | 48 hours | To evaluate the cytotoxic effects of LCL161 and paclitaxel, results showed that paclitaxel significantly reduced cell viability, while LCL161 alone had minimal effect. | PMC5062899 |
| EMT6 cells | 100 nM | 2 hours | To test the effect of LCL161 on EMT6 cell viability, results showed that LCL161 significantly reduced cell viability. | PMC5570934 |
| BMDMs | 50 nM, 250 nM, 1000 nM | 24 hours | To test the effect of LCL161 on IFN-γ and TNF-α expression in BMDMs, results showed that LCL161 increased the expression of these cytokines. | PMC5570934 |
| A549 | 25 μM | 24 h | To evaluate the effect of LCL161 on A549 cell elongation, invasion and migration, it was found that LCL161 stimulated A549 cell elongation, invasion and migration at non-toxic concentrations. | PMC7667862 |
| H1299 | 10 μM | 24 h | To evaluate the effect of LCL161 on H1299 cell elongation, invasion and migration, it was found that LCL161 stimulated H1299 cell elongation, invasion and migration at non-toxic concentrations. | PMC7667862 |
| μM.1S cells | 5 µM | 24 hours | LCL161 and LBH589 synergistically induced apoptosis in μM.1S cells | PMC8679669 |
| U266 cells | 5 µM | 24 hours | LCL161 and LBH589 synergistically induced apoptosis in U266 cells | PMC8679669 |
| SW480 cells | 10 μM | 1 hour | LCL161 disrupted the association of BIRC2 with H3 and induced BIRC2 degradation | PMC10702411 |
| human macrophages | 10 μM | 24 hours | LCL161 induced BIRC2 degradation and increased IL-6 and RANTES expression | PMC10702411 |
In Vivo:
| Administration | Dosage | Frequency | Description | References |
| Nude mice | H460 subcutaneous tumor model | Intraperitoneal injection | 100 mg/d | Daily, for 10 months | To evaluate the antitumor efficacy of LCL161 and paclitaxel combination, results showed that the combination significantly inhibited tumor growth with minimal toxicity. | PMC5062899 |
| mice | EMT6 breast tumor model | oral | 5 mM | 1 hour and 18 hours | To test the effect of LCL161 combined with VSVΔM51 on EMT6 tumors, results showed that the combination therapy significantly enhanced CD8+T cell-mediated anti-tumor immune responses. | PMC5570934 |
| BALB/c nude mice | Lung cancer model | Intraperitoneal injection | 10 mg/kg LCL161 and/or 20 mg/kg paclitaxel | Every two days for three weeks | To evaluate the inhibitory effect of OTUD7B on LCL161-induced lung cancer cell metastasis in vivo, it was found that OTUD7B inhibited LCL161-induced intrapulmonary metastasis of lung cancer cells. | PMC7667862 |
| Mice | 5TGM1 murine multiple myeloma model | Intraperitoneal injection | 50 mg/kg | every 72 hours, total of four times | Combined LCL161 and LBH589 treatment significantly increased survival in mice | PMC8679669 |
| mice | oral (PO), intravenous (IV), intraperitoneal (IP) | 2 mg/kg | Every 2 days for 3 weeks | To evaluate the pharmacokinetic properties of 142D6, the results showed that 142D6 is orally bioavailable with an oral bioavailability of 36%. | PMC10291551 | |
| NSG mice | LuCaP 170.3 PDX model | Oral | 30 mg/kg (PO and IP), 10 mg/kg (IV) | single dose, duration of 24 hours | To evaluate the therapeutic efficacy of LCL161 in HNF1A+ mCRPC models. Results showed that LCL161 monotherapy significantly inhibited tumor growth in the HNF1A+ LuCaP 170.3 model, while it had minimal effect in the HNF1A- LuCaP 170.2 model. | PMC11722106 |
| BALB/c mice | 4T1H-2Kb KO tumor model | Intravenous injection | 100 nM | 4 hours | LMN significantly inhibited the growth of 4T1H-2Kb KO tumors and prolonged the survival of mice. | PMC11252456 |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT01098838 | Advanced Solid Tumors | PHASE1 | COMPLETED | 2025-01-11 | UNC/ Lineberger Comprehensive … More >>Cancer Center Dept. of LinbergerCancerCtr(2), Chapel Hill, North Carolina, 27599-7295, United States|Fox Chase Cancer Center, Philadelphia, Pennsylvania, 19111-2497, United States|Sarah Cannon Research Institute DeptofSarahCannonRes.Inst. (2), Nashville, Tennessee, 37203, United States Less << |
Protocol
| Bio Calculators | ||||
| Preparing Stock Solutions |  |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.00mL 0.40mL 0.20mL |
9.99mL 2.00mL 1.00mL |
19.97mL 3.99mL 2.00mL |
|
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