NVP-LCQ195

Product Name: NVP-LCQ195
CAS No.: 902156-99-4
Chemical Name: NVP-LCQ195
Synonyms: LCQ-195;LCQ 195;AT-9311;AT 9311;NVP-LCQ195;NVP-LCQ195 (AT9311;NVP-LCQ195, 10 mM in DMSO;NVP-LCQ195 (AT9311; LCQ195);NVP-LCQ195;LCQ-195;AT-9311;NVP LCQ195;LCQ-195;AT-9311;NVP LCQ195;LCQ 195;AT9311;AT 9311
CBNumber: CB12628205
Molecular Formula: C17H19Cl2N5O4S
Formula Weight: 460.33486
MOL File: 902156-99-4.mol

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NVP-LCQ195 Property

Density: 1.57±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: insoluble in H2O; ≥152.4 mg/mL in DMSO; ≥3.28 mg/mL in EtOH with gentle warming and ultrasonic
form: solid
pka: 11.10±0.70(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0840
Product name: NVP-LCQ195
Purity: 99.80%
Packaging: 5mg
Price: $230
Updated: 2021/12/16

ApexBio Technology

Product number: A3676
Product name: NVP-LCQ195
Packaging: 5mg
Price: $256
Updated: 2021/12/16

ChemScene

Product number: CS-0840
Product name: NVP-LCQ195
Purity: 99.80%
Packaging: 10mg
Price: $330
Updated: 2021/12/16

ApexBio Technology

Product number: A3676
Product name: NVP-LCQ195
Packaging: 10mg
Price: $359
Updated: 2021/12/16

Crysdot

Product number: CD31000341
Product name: NVP-LCQ195
Purity: 98+%
Packaging: 5mg
Price: $166
Updated: 2021/12/16

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NVP-LCQ195 Chemical Properties,Usage,Production

Uses

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.

IC 50

Cdk5/p25: 1 nM (IC₅₀); CDK5/p35: 1 nM (IC₅₀); Cdk1/cyclin B: 2 nM (IC₅₀); cdk2/cyclin A: 2 nM (IC₅₀); CDK2/cyclinE: 5 nM (IC₅₀); CDK9/cyclinT1: 15 nM (IC₅₀); CDK3/Cyclin E: 42 nM (IC₅₀); cdk6/cyclin D3: 187 nM (IC₅₀); CDK7/Cyclin H/MAT1: 3564 nM (IC₅₀)

References

[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 Feb;152(4):420-32. DOI:10.1111/j.1365-2141.2010.08427.x

NVP-LCQ195 Preparation Products And Raw materials

Raw materials

Preparation Products

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NVP-LCQ195 Suppliers

China 73 United States 8 Global 81

Nanjing Chemlin Chemical Co., Ltd

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NVP-LCQ195, 10 mM in DMSO

4-[(2,6-dichlorobenzoyl)amino]-N-(1-methylsulfonylpiperidin-4-yl)-1H-pyrazole-5-carboxamide

902156-99-4

C17H19Cl2N5O4S