NVP-LCQ195CDK1/CDK2/CDK5 inhibitor CAS# 902156-99-4 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 902156-99-4 | SDF | Download SDF |
| PubChem ID | 11655534 | Appearance | Powder |
| Formula | C17H19Cl2N5O4S | M.Wt | 460.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | LCQ-195; AT9311 | ||
| Solubility | DMSO : ≥ 100 mg/mL (217.24 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[(2,6-dichlorobenzoyl)amino]-N-(1-methylsulfonylpiperidin-4-yl)-1H-pyrazole-5-carboxamide | ||
| SMILES | CS(=O)(=O)N1CCC(CC1)NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl | ||
| Standard InChIKey | CCUXEBOOTMDSAM-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H19Cl2N5O4S/c1-29(27,28)24-7-5-10(6-8-24)21-17(26)15-13(9-20-23-15)22-16(25)14-11(18)3-2-4-12(14)19/h2-4,9-10H,5-8H2,1H3,(H,20,23)(H,21,26)(H,22,25) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.
IC50 Value: 1 nM(CDK5/p25 and CDK5/p35); 2 nM(CDK1/cyclinB and CDK2/cyclinA); 5 nM(CDK2/cyclinE); 42 nM(CDK3/cyclinE)
Target: CDKs
LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-lmol/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. 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. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM. References: | |||||
NVP-LCQ195 Dilution Calculator
NVP-LCQ195 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1724 mL | 10.8618 mL | 21.7235 mL | 43.4471 mL | 54.3089 mL |
| 5 mM | 0.4345 mL | 2.1724 mL | 4.3447 mL | 8.6894 mL | 10.8618 mL |
| 10 mM | 0.2172 mL | 1.0862 mL | 2.1724 mL | 4.3447 mL | 5.4309 mL |
| 50 mM | 0.0434 mL | 0.2172 mL | 0.4345 mL | 0.8689 mL | 1.0862 mL |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2172 mL | 0.4345 mL | 0.5431 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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NVP-LCQ195 is a pan-inhibitor of CDKs [1].
Cyclin-dependent kinases (CDKs) are a family of protein kinases and play an important role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells.
In vitro kinase activity assays, NVP-LCQ195 blocks the activity of CDK1/cyclin B and CDK2/cyclin A, CDK2/cyclin E, as well as CDK5 (both CDK5 p25 and CDK5 p35) with IC50 value of 2 nM, 2 nM, 5 nM and 1 nM, respectively. Also, it inhibited CLK3 and CHEK2 (CHK2), CDK3/cyclin E, CDK9/cyclin T1, CDK7/cyclin H and CDK6/cyclin D3. In MM.1S cells, NVP-LCQ195 (2 μM) increased the percentage of cells in S and G2/M phases early, followed by an increase in sub-G1 population. Also, NVP-LCQ195 suppressed the expression of transcription factors including myc, IRF4 and XBP-1 [1].
In bortezomib-treated MM patients, NVP-LCQ195 suppressed high expression of genes and significantly increased progression-free and overall survival [1].
Reference:
[1]. McMillin DW, Delmore J, Negri J, et al. Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications. Br J Haematol, 2011, 152(4): 420-432.
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Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications.[Pubmed:21223249]
Br J Haematol. 2011 Feb;152(4):420-32.
Cell cycle regulators, such as cyclin-dependent kinases (CDKs), are appealing targets for multiple myeloma (MM) therapy given the increased proliferative rates of tumour cells in advanced versus early stages of MM. We hypothesized that a multi-targeted CDK inhibitor with a different spectrum of activity compared to existing CDK inhibitors could trigger distinct molecular sequelae with therapeutic implications for MM. We therefore studied the small molecule heterocyclic compound NVP-LCQ195/AT9311 (LCQ195), which inhibits CDK1, CDK2 and CDK5, as well as CDK3 and CDK9. LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-mumol/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-1alpha, IRF4. 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. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM.
