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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
NVP-LCQ195 (formerly also known as AT9311; AT-9311; LCQ195; LCQ-195) is a novel and potent small molecule heterocyclic inhibitor of cyclin-dependent kinases CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. Even at sub-μmol/l concentrations, LCQ195 caused MM cells to enter a cell cycle arrest and ultimately undergo apoptosis. It also preserved non-cancerous cells and eliminated the shield that the bone marrow milieu's stroma or cytokines provided for MM cells. Given the higher rates of tumor cell proliferation in advanced MM compared to early stages, cell cycle regulators, such as cyclin-dependent kinases (CDKs), are attractive targets for multiple myeloma (MM) therapy.
Targets |
Cdk5/p25 (IC50 = 1 nM); CDK5/p35 (IC50 = 1 nM); Cdk1/cyclin B (IC50 = 2 nM); cdk2/cyclin A (IC50 = 2 nM); CDK2/cyclinE (IC50 = 5 nM); CDK9/cyclinT1 (IC50 = 15 nM); CDK3/Cyclin E (IC50 = 42 nM); cdk6/cyclin D3 (IC50 = 187 nM); CDK7/Cyclin H/MAT1 (IC50 = 3564 nM)
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References |
Molecular Formula |
C17H19CL2N5O4S
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Molecular Weight |
460.3349
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Exact Mass |
459.05
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Elemental Analysis |
C, 44.36; H, 4.16; Cl, 15.40; N, 15.21; O, 13.90; S, 6.96
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CAS # |
902156-99-4
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Related CAS # |
902156-99-4
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Appearance |
Solid powder
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SMILES |
CS(=O)(=O)N1CCC(CC1)NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl
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InChi Key |
CCUXEBOOTMDSAM-UHFFFAOYSA-N
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InChi Code |
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)
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Chemical Name |
4-[(2,6-dichlorobenzoyl)amino]-N-(1-methylsulfonylpiperidin-4-yl)-1H-pyrazole-5-carboxamide
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Synonyms |
NVP-LCQ-195; NVP-LCQ195; NVP-LCQ 195; LCQ 195; LCQ-195; LCQ195; AT9311; AT-9311; AT 9311
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 66.7~92 mg/mL (144.8~199.9 mM)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1724 mL | 10.8618 mL | 21.7235 mL | |
5 mM | 0.4345 mL | 2.1724 mL | 4.3447 mL | |
10 mM | 0.2172 mL | 1.0862 mL | 2.1724 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
In vitrokinase activity in the presence of LCQ195.Br J Haematol.2011 Feb;152(4):420-32. th> |
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LCQ195 cause cell cycle arrest and cell death.Br J Haematol.2011 Feb;152(4):420-32. td> |
Treatment of MM.1S cells with LCQ195 leads to distinct changes in transcriptional signatures of activation of key molecular pathways in tumor cell pathophysiology.Br J Haematol.2011 Feb;152(4):420-32. td> |
Activity of LCQ195 on MM cells.Br J Haematol.2011 Feb;152(4):420-32. th> |
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LCQ195 enhances the anti-MM activity of dexamethasonein vitro.Br J Haematol.2011 Feb;152(4):420-32. td> |
LCQ195 treatment induces a transcriptional response of genes which correlate with clinical outcome. td> |