1. Cell Cycle/DNA Damage
  2. CDK
  3. SEL120-34A

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

SEL120-34A 構造式

CAS 番号 : 1609522-33-9

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 228 在庫あり
Solution
10 mM * 1 mL in DMSO USD 228 在庫あり
Solid
5 mg $208 在庫あり
10 mg $270 在庫あり
25 mg $466 在庫あり
50 mg $715 在庫あり
100 mg $1065 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 8 publication(s) in Google Scholar

Other Forms of SEL120-34A:

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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 μM
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 μM
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 μM
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 μM
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
< 1000 nM
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 μM
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
< 1000 nM
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 μM
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 μM
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 μM
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 μM
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 nM
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 nM
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
43.77 nM
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
< 1000 nM
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 nM
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 μM
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]
体外実験

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.

体内実験

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.

分子量

414.14

分子式

C15H18Br2N4

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

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

一般には略語で表示されます:C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
参考文献

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.

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
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  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
SEL120-34A
製品番号:
HY-111388
数量:
MCE 日本正規代理店: