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

Cat. No.: HY-15241 Purity: 98.91%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 902156-99-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 135	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 135	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 123	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 354	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 741	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

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

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

Appearance

Solid

Color

White to off-white

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	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 66.67 mg/mL (144.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.91%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (253 KB) LCMS (118 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1724 mL	10.8618 mL	21.7235 mL	54.3089 mL
	5 mM	0.4345 mL	2.1724 mL	4.3447 mL	10.8618 mL
	10 mM	0.2172 mL	1.0862 mL	2.1724 mL	5.4309 mL
	15 mM	0.1448 mL	0.7241 mL	1.4482 mL	3.6206 mL
	20 mM	0.1086 mL	0.5431 mL	1.0862 mL	2.7154 mL
	25 mM	0.0869 mL	0.4345 mL	0.8689 mL	2.1724 mL
	30 mM	0.0724 mL	0.3621 mL	0.7241 mL	1.8103 mL
	40 mM	0.0543 mL	0.2715 mL	0.5431 mL	1.3577 mL
	50 mM	0.0434 mL	0.2172 mL	0.4345 mL	1.0862 mL
	60 mM	0.0362 mL	0.1810 mL	0.3621 mL	0.9051 mL
	80 mM	0.0272 mL	0.1358 mL	0.2715 mL	0.6789 mL
	100 mM	0.0217 mL	0.1086 mL	0.2172 mL	0.5431 mL

NVP-LCQ195 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NVP-LCQ195902156-99-4LCQ-195 AT9311LCQ195LCQ 195AT9311AT 9311AT-9311CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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