LY2409881 trihydrochloride
- CAS NO.:946518-60-1
- Empirical Formula: C24H30Cl2N6OS
- Molecular Weight: 521.51
- MDL number: MFCD28900676
- Update Date: 2024-11-19 20:33:22
What is LY2409881 trihydrochloride?
The Uses of LY2409881 trihydrochloride
2-[5-Chloro-2-[[3-(4-methylpiperazin-1-yl)propyl]amino]pyrimidin-4-yl]benzo[b]thiophene-4-carboxamide N-cyclopropyl Trihydrochloride is an inhibitor of IkB-kinase (IKK2). Small molecules that inhibits IkB-kinase and NF-κB pathways are potential anti-inflammatory drug candidate.
Biological Activity
ly2409881 is a potent and selective inhibitor of ikk2 with ic50 value of 30 nm [1].iκb kinase β (ikk2) is an enzyme that serves as a subunit of iκb kinase, which is involved in the cytokine-activated immune responses. ikk2 activates nuclear factor kappa-b kinase (nf-κb).ly2409881 is a selective ikk2 inhibitor and exhibited >10-fold selectivity over other common kinases and ikk1. in the ovarian cancer cell line skov3, ly2409881 showed moderate cytotoxicity. while coadministration of ly2409881 and tnfɑ significantly induced cells death, which suggested ly2409881 inhibited nf-κb mediated antiapoptotic signals in a tnfɑ-dependent way. in the dlbcl cell line ly10, ly2409881 (10 μm) inhibited tnfɑ-dependent phosphorylation of iκb. in the dlbcl cell line sudhl2, ly2409881 (10 μm) inhibited the nuclear signals of p50 and nf-κb. also, ly2409881 induced apoptosis in a concentration-dependent way [1].in scid-beige mice bearing ly10 cell-derived tumors, ly2409881 (50, 100 and 200 mg/kg) significantly inhibited tumor growth [1].
References
[1]. deng c, lipstein m, rodriguez r, et al. the novel ikk2 inhibitor ly2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of nf-κb. clin cancer res, 2015, 21(1): 134-145.
Properties of LY2409881 trihydrochloride
storage temp. | Store at -20°C |
solubility | ≥59.4 mg/mL in DMSO with ultrasonic; insoluble in EtOH; insoluble in H2O |
form | solid |
color | Light yellow to yellow |
Safety information for LY2409881 trihydrochloride
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation |
Precautionary Statement Codes |
P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. P332+P313:IF SKIN irritation occurs: Get medical advice/attention. P337+P313:IF eye irritation persists: Get medical advice/attention. |
Computed Descriptors for LY2409881 trihydrochloride
New Products
4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium THOMAIND PAPER PH 2.0 TO 4.5 1 BOX BUFFER CAPSULE PH 9.2 - 10 CAP SODIUM CHLORIDE 0.1N CVS ALLOXAN MONOHYDRATE 98% PLATINUM 0.5% ON 3 MM ALUMINA PELLETS (TYPE 73) LITHIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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