PROTAC CDK2/9 Degrader-1

Name: PROTAC CDK2/9 Degrader-1
Brand: MedChemExpress
SKU: HY-130709
Rating: 4.5 (1 reviews)

Cat. No.: HY-130709 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC₅₀=62 nM) and CDK9 (DC₅₀=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC₅₀=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.

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

PROTAC CDK2/9 Degrader-1 Chemical Structure

CAS No. : 2408641-24-5

Size	Price	Stock	Quantity
5 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3750	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CDK2

62 nM (DC₅₀)

CDK9

33 nM (DC₅₀)

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	14.5 nM Compound: F3	Inhibition of tracer K10 binding to NanoLuc-CDK9/Cyclin T1 (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay Inhibition of tracer K10 binding to NanoLuc-CDK9/Cyclin T1 (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay	[PMID: 31846828]
HEK293	IC₅₀	7.42 nM Compound: F3	Inhibition of tracer K10 binding to NanoLuc-CDK2/Cyclin A (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay Inhibition of tracer K10 binding to NanoLuc-CDK2/Cyclin A (unknown origin) expressed in human HEK293 cells after 1 hr in presence of ATP by NanoBRET assay	[PMID: 31846828]
L02	IC₅₀	7.99 μM Compound: F3	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 5 days by CCK-8 assay	[PMID: 31846828]
PC-3	IC₅₀	0.12 μM Compound: F3	Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay Antiproliferative activity against AR-negative human PC3 cells assessed as reduction in cell viability after 5 days by CCK8 assay	[PMID: 31846828]

In Vitro

PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase^[1].
PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells^[1].
PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression^[1].
PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC₅₀ as 7.42 nM and 14.50 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	500 nM
Incubation Time:	2, 4, 8, 16, 24 hours
Result:	Down-regulated the Mcl-1 protein level in PC-3 cells.

Western Blot Analysis^[1]

Cell Line:	PC-3 cells
Concentration:	0.25, 1, 3 μM
Incubation Time:	48 hours
Result:	Induced cell cycle blockage at the G2/M phase.

Molecular Weight

815.84

Formula

C₄₀H₄₁N₁₃O₇

CAS No.

2408641-24-5

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=NNC=C1NC2=C3C(NC=C3)=NC=N2)NC4=CC=C(CN5CCN(C(CCC(NCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O)CC5)C=C4

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 : 50 mg/mL (61.29 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	1.2257 mL	6.1287 mL	12.2573 mL
5 mM	0.2451 mL	1.2257 mL	2.4515 mL
10 mM	0.1226 mL	0.6129 mL	1.2257 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: 5 mg/mL (6.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

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: 99.85%

Select Batch:

Data Sheet (271 KB) SDS (252 KB)

COA (245 KB) HNMR (183 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

References

[1]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.2257 mL	6.1287 mL	12.2573 mL	30.6433 mL
	5 mM	0.2451 mL	1.2257 mL	2.4515 mL	6.1287 mL
	10 mM	0.1226 mL	0.6129 mL	1.2257 mL	3.0643 mL
	15 mM	0.0817 mL	0.4086 mL	0.8172 mL	2.0429 mL
	20 mM	0.0613 mL	0.3064 mL	0.6129 mL	1.5322 mL
	25 mM	0.0490 mL	0.2451 mL	0.4903 mL	1.2257 mL
	30 mM	0.0409 mL	0.2043 mL	0.4086 mL	1.0214 mL
	40 mM	0.0306 mL	0.1532 mL	0.3064 mL	0.7661 mL
	50 mM	0.0245 mL	0.1226 mL	0.2451 mL	0.6129 mL
	60 mM	0.0204 mL	0.1021 mL	0.2043 mL	0.5107 mL