SEL120-34A

Name: SEL120-34A
Brand: MedChemExpress
SKU: HY-111388
Rating: 5.0 (8 reviews)

Art. -Nr.: HY-111388 Reinheit: 99.49%: Data Sheet
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SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

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SEL120-34A Chemische Struktur

CAS. Nr. : 1609522-33-9

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 8 publication(s) in Google Scholar

Other Forms of SEL120-34A:

Romaciclib monohydrochloride In-stock
Romaciclib hydrochloride In-stock

8 Publications Citing Use of MCE SEL120-34A

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle CDK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

SEL120-34A is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

IC₅₀ & Target^[1]

CDK8/CycC

4.4 nM (IC₅₀)

CDK19/CycC

10.4 nM (IC₅₀)

CDK9/cycT

1070 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	GI₅₀	5.9 3 Compound: SEL120-34A	Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
A-375	GI₅₀	5.9 3 Compound: SEL120-34A	Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A-375 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
A549	GI₅₀	12.06 3 Compound: SEL120-34A	Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
A549	GI₅₀	12.06 3 Compound: SEL120-34A	Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
GES1	GI₅₀	55.3 3 Compound: SEL120-34A	Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
GES1	GI₅₀	55.3 3 Compound: SEL120-34A	Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human GES1 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HCT-116	GI₅₀	11.3 3 Compound: SEL120-34A	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HCT-116	GI₅₀	11.3 3 Compound: SEL120-34A	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HL-60	GI₅₀	<1 3 Compound: 2; SEL120-34A	Growth inhibition of human HL60 cells by alamar blue assay Growth inhibition of human HL60 cells by alamar blue assay	[PMID: 29266937]
HL-60	GI₅₀	< 1000 1 Compound: 2; SEL120-34A	Growth inhibition of human HL60 cells by alamar blue assay Growth inhibition of human HL60 cells by alamar blue assay	[PMID: 29266937]
HT-29	GI₅₀	33.8 3 Compound: SEL120-34A	Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
HT-29	GI₅₀	33.8 3 Compound: SEL120-34A	Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human HT-29 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
KG-1	GI₅₀	<1 3 Compound: 2; SEL120-34A	Growth inhibition of human KG1 cells by alamar blue assay Growth inhibition of human KG1 cells by alamar blue assay	[PMID: 29266937]
KG-1	GI₅₀	< 1000 1 Compound: 2; SEL120-34A	Growth inhibition of human KG1 cells by alamar blue assay Growth inhibition of human KG1 cells by alamar blue assay	[PMID: 29266937]
MDA-MB-231	GI₅₀	9.6 3 Compound: SEL120-34A	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MDA-MB-231	GI₅₀	9.6 3 Compound: SEL120-34A	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MGC-803	GI₅₀	16.26 3 Compound: SEL120-34A	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MGC-803	GI₅₀	16.26 3 Compound: SEL120-34A	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MOLM-13	GI₅₀	0.02 3 Compound: SEL120-34A	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MOLM-13	GI₅₀	0.02 3 Compound: SEL120-34A	Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MOLM-13 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MV4-11	GI₅₀	0.07 3 Compound: SEL120-34A	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MV4-11	GI₅₀	0.07 3 Compound: SEL120-34A	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
MV4-11	GI₅₀	< 1000 1 Compound: 2; SEL120-34A	Growth inhibition of human MV4-11 cells by alamar blue assay Growth inhibition of human MV4-11 cells by alamar blue assay	[PMID: 29266937]
MV4-11	GI₅₀	<1 3 Compound: 2; SEL120-34A	Growth inhibition of human MV4-11 cells by alamar blue assay Growth inhibition of human MV4-11 cells by alamar blue assay	[PMID: 29266937]
MV4-11	IC₅₀	248.75 1 Compound: RVU120; SEL120	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay	[PMID: 37029334]
MV4-11	IC₅₀	248.75 1 Compound: RVU120; SEL120	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 10 days and replacement with fresh media with compounds on day 5 by CTG assay	[PMID: 37029334]
OCI-AML2	GI₅₀	<1 3 Compound: 2; SEL120-34A	Growth inhibition of human OCI-AML2 cells by alamar blue assay Growth inhibition of human OCI-AML2 cells by alamar blue assay	[PMID: 29266937]
MV4-11	IC₅₀	43.77 1 Compound: RVU120	Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MV4-11 cells incubated for 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 38690856]
OCI-AML-3	GI₅₀	<1 3 Compound: 2; SEL120-34A	Growth inhibition of human OCI-AML3 cells by alamar blue assay Growth inhibition of human OCI-AML3 cells by alamar blue assay	[PMID: 29266937]
SW480	GI₅₀	17.7 3 Compound: SEL120-34A	Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]
OCI-AML-3	GI₅₀	< 1000 1 Compound: 2; SEL120-34A	Growth inhibition of human OCI-AML3 cells by alamar blue assay Growth inhibition of human OCI-AML3 cells by alamar blue assay	[PMID: 29266937]
OCI-AML2	GI₅₀	< 1000 1 Compound: 2; SEL120-34A	Growth inhibition of human OCI-AML2 cells by alamar blue assay Growth inhibition of human OCI-AML2 cells by alamar blue assay	[PMID: 29266937]
SW480	GI₅₀	17.7 3 Compound: SEL120-34A	Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay Antiproliferative activity against human SW480 cells incubated for 48 hrs by CCK8 assay	[PMID: 36889252]

In Vitro

SEL120-34A is a selective, ATP-competitive CDK8 inhibitor, with IC₅₀ of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively. SEL120-34A shows no obvious inhibition on CDK1, 2, 4, 6, 5, 7, and only weakly suppresses CDK9 (IC₅₀, 1070 nM). SEL120-34A is active against a panel of AML cell lines (GI₅₀<1 μM), such as SKNO-1, KG-1, HEL-60, MOLM-16, MV-4-11, OciAML-2, MOLM-6 and OciAML-3 cells, consistent with the effective inhibition range of STAT1 S727 and STAT5 S726^[1].

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

In Vivo

SEL120-34A (30, 60 mg/kg, p.o.) inhibits the growth of tumor in mice bearing MV4-11 cancer cells, and also arrests the growth of KG-1-derived tumors at 30 mg/kg via oral administration^[1].

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

Molekulargewicht

414.14

Formel

C₁₅H₁₈Br₂N₄

CAS. Nr.

1609522-33-9

Appearance

Solid

Color

White to off-white

SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (48.29 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	2.4146 mL	12.0732 mL	24.1464 mL
5 mM	0.4829 mL	2.4146 mL	4.8293 mL
10 mM	0.2415 mL	1.2073 mL	2.4146 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.

Molaritätsrechner
Verdünnungsrechner

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 Dissolution Calculator

Please enter the basic information of animal experiments:

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Calculation results:

Working solution concentration: mg/mL

Reinheit & Dokumentation

Purity: 99.49%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (251 KB) HNMR (414 KB) RP-HPLC (257 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

Verweise

[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	1 mM	2.4146 mL	12.0732 mL	24.1464 mL	60.3661 mL
	5 mM	0.4829 mL	2.4146 mL	4.8293 mL	12.0732 mL
	10 mM	0.2415 mL	1.2073 mL	2.4146 mL	6.0366 mL
	15 mM	0.1610 mL	0.8049 mL	1.6098 mL	4.0244 mL
	20 mM	0.1207 mL	0.6037 mL	1.2073 mL	3.0183 mL
	25 mM	0.0966 mL	0.4829 mL	0.9659 mL	2.4146 mL
	30 mM	0.0805 mL	0.4024 mL	0.8049 mL	2.0122 mL
	40 mM	0.0604 mL	0.3018 mL	0.6037 mL	1.5092 mL

SEL120-34A 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:

SEL120-34A1609522-33-9CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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SEL120-34A

Kundenbewertung

Other Forms of SEL120-34A:

SEL120-34A Related Antibodies

8 Publications Citing Use of MCE SEL120-34A

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle CDK Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

SEL120-34A Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

SEL120-34A Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

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SAFETY DATA SHEET (SDS)

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