SEL120-34A monohydrochloride

Name: SEL120-34A monohydrochloride
Brand: MedChemExpress
SKU: HY-111388A
Rating: 5.0 (5 reviews)

Cat. No.: HY-111388A Purity: 99.29%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.

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

SEL120-34A monohydrochloride Chemical Structure

CAS No. : 2443816-41-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 176	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 176	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 820	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of SEL120-34A monohydrochloride:

SEL120-34A hydrochloride In-stock
SEL120-34A Get quote

5 Publications Citing Use of MCE SEL120-34A monohydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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]

CDK8/CycC

4.4 nM (IC₅₀)

CDK19/CycC

10.4 nM (IC₅₀)

CDK9/cycT

1070 nM (IC₅₀)

In Vitro

SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7^[1].
SEL120-34A (1.6 nM-5 μM) inhibits the growth of STAT5 S726 positive KG-1 AML cells, but is not cytotoxic to S726 negative MOLM13 AML cells^[1].
SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726, decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression^[1].

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

In Vivo

SEL120-34A monohydrochloride (30, 60 mg/kg, p.o. once every day) inhibits growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days^[1].

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

Molecular Weight

450.60

Formula

C₁₅H₁₉Br₂ClN₄

CAS No.

2443816-41-7

Appearance

Solid

Color

White to off-white

SMILES

CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (110.96 mM; Need ultrasonic)

DMSO : 16.67 mg/mL (37.00 mM; ultrasonic and warming and heat to 60°C; 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	2.2193 mL	11.0963 mL	22.1926 mL
5 mM	0.4439 mL	2.2193 mL	4.4385 mL
10 mM	0.2219 mL	1.1096 mL	2.2193 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: ≥ 1.67 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.67 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 14.29 mg/mL (31.71 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.29%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (253 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO / H₂O	1 mM	2.2193 mL	11.0963 mL	22.1926 mL	55.4816 mL
	5 mM	0.4439 mL	2.2193 mL	4.4385 mL	11.0963 mL
	10 mM	0.2219 mL	1.1096 mL	2.2193 mL	5.5482 mL
	15 mM	0.1480 mL	0.7398 mL	1.4795 mL	3.6988 mL
	20 mM	0.1110 mL	0.5548 mL	1.1096 mL	2.7741 mL
	25 mM	0.0888 mL	0.4439 mL	0.8877 mL	2.2193 mL
	30 mM	0.0740 mL	0.3699 mL	0.7398 mL	1.8494 mL
H₂O	40 mM	0.0555 mL	0.2774 mL	0.5548 mL	1.3870 mL
	50 mM	0.0444 mL	0.2219 mL	0.4439 mL	1.1096 mL
	60 mM	0.0370 mL	0.1849 mL	0.3699 mL	0.9247 mL
	80 mM	0.0277 mL	0.1387 mL	0.2774 mL	0.6935 mL
	100 mM	0.0222 mL	0.1110 mL	0.2219 mL	0.5548 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.