1. Cell Cycle/DNA Damage
  2. CDK
  3. NVP-LCQ195

NVP-LCQ195 (Synonyms: LCQ-195; AT9311)

Cat. No.: HY-15241 Purity: 98.99%
Handling Instructions

NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.

For research use only. We do not sell to patients.

NVP-LCQ195 Chemical Structure

NVP-LCQ195 Chemical Structure

CAS No. : 902156-99-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 337 In-stock
Estimated Time of Arrival: December 31
5 mg USD 306 In-stock
Estimated Time of Arrival: December 31
10 mg USD 430 In-stock
Estimated Time of Arrival: December 31
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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.

IC50 & Target[1]

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)

Molecular Weight

460.33

Formula

C₁₇H₁₉Cl₂N₅O₄S

CAS No.

902156-99-4

SMILES

CS(=O)(N1CCC(NC(C2=C(NC(C3=C(Cl)C=CC=C3Cl)=O)C=NN2)=O)CC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (217.24 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NVP-LCQ195LCQ-195AT9311LCQ195LCQ 195AT 9311AT-9311CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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Product name:
NVP-LCQ195
Cat. No.:
HY-15241
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