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NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $40 | In Stock | |
5 mg | $98 | In Stock | |
10 mg | $148 | In Stock | |
25 mg | $283 | In Stock | |
50 mg | $416 | In Stock | |
100 mg | $593 | In Stock | |
200 mg | $783 | In Stock | |
1 mL x 10 mM (in DMSO) | $100 | In Stock |
Description | NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM). |
Targets&IC50 | CDK2-CyclinE:5 nM, CDK9-CyclinT1:15 nM, CDK1-CyclinB:2 nM, CDK7-CyclinH-MAT1:3564 nM, CDK5-p35:1 nM, CDK6-CyclinD3:187 nM, CDK5-p25:1 nM, CDK2-CyclinA:2 nM, CDK3-CyclinE:42 nM |
In vitro | NVP-LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-1 mol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. In MM cells, LCQ195 triggered decreased amplitude of transcriptional signatures associated with oncogenesis, drug resistance and stem cell renewal, including signatures of activation of key transcription factors for MM cells e.g. myc, HIF-1a, IRF4[1]. |
In vivo | Bortezomib-treated MM patients whose tumours had high baseline expression of genes suppressed by LCQ195 had significantly shorter progression-free and overall survival than those with low levels of these transcripts in their MM cells[1]. |
Alias | LCQ-195, AT9311 |
Molecular Weight | 460.33 |
Formula | C17H19Cl2N5O4S |
Cas No. | 902156-99-4 |
Smiles | CS(=O)(=O)N1CCC(CC1)NC(=O)c1[nH]ncc1NC(=O)c1c(Cl)cccc1Cl |
Relative Density. | 1.57 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (217.24 mM) H2O: Insoluble | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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