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Alsterpaullone CDK inhibitor

Name: Alsterpaullone
Brand: Selleck Chemicals
SKU: S0354
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0354

Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. This compound also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. It induces apoptosis by activation of caspase-9. This chemical has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.

Chemical Structure

Molecular Weight: 293.28

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Quality Control

Batch: S035401 DMSO]25 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.81%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.81

Related Targets	HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase Casein Kinase
Other CDK Inhibitors	Ro-3306 JNJ-7706621 AZD4573 Enitociclib (BAY 1251152) SEL120 (SEL120-34A) hydrochloride Samuraciclib (ICEC0942) hydrochloride ON123300 AS2863619 PF-07220060 (CDK4/6-IN-6) SY-5609 INX-315 Tagtociclib (PF-07104091)

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (85.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	293.28	Formula	C₁₆H₁₁N₃O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	237430-03-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Alp, 9-Nitropaullone, NSC 705701			Smiles	C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)[N+](=O)[O-]

Mechanism of Action

Targets/IC₅₀/Ki	caspase-9 GSK-3α (Cell-free assay) 4 nM GSK-3β (Cell-free assay) 4 nM CDK2/cyclin A (Cell-free assay) 15 nM CDK1/cyclin B (Cell-free assay) 35 nM CDK5/p35 (Cell-free assay) 40 nM CDK2/cyclin E (Cell-free assay) 200 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/10998059/ [2] https://pubmed.ncbi.nlm.nih.gov/12669310/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03160430	Not yet recruiting	Kidney Failure Chronic	Resverlogix Corp	November 22 2024	Phase 1\|Phase 2
NCT06377293	Not yet recruiting	End-Stage Kidney Disease	Far Eastern Memorial Hospital	November 2024	Not Applicable
NCT06405555	Not yet recruiting	Heart Failure With Reduced Ejection Fraction\|Hypotension\|LV Dysfunction	Ottawa Heart Institute Research Corporation	August 1 2024	Phase 2\|Phase 3
NCT06398002	Not yet recruiting	Secondary Hyperparathyroidism\|End-stage Kidney Disease	Iain Bressendorff\|Herlev Hospital	August 1 2024	Phase 2
NCT06383403	Not yet recruiting	Primary Biliary Cholangitis	Ipsen	July 1 2024	Phase 3
NCT06095986	Not yet recruiting	Primary Sclerosing Cholangitis	Galmed Research and Development Ltd.\|Virginia Commonwealth University\|Galmed Pharmaceuticals Ltd	June 2024	Phase 2

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Handling Instructions

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