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製品番号: HY-176736

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CDK9-IN-40

CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC₅₀ of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₂₁H₂₆N₈S
分子量:422.55

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

CDK9-IN-40 構造式

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

CDK9

5.5 nM (IC₅₀)

CDK アイソフォーム固有の製品をすべて表示 :

体外実験

CDK9-IN-40 (Compound 8e) (1.0 μM, 48 h) exhibits the highest inhibitory activities against CDK9 (99% inhibition, IC₅₀ = 5.5 nM) and shows over 180 and 75-fold selectivity for CDK9 versus CDK1 and CDK2, respectively^[1].
CDK9-IN-40 (1.8 μM-3.0 μM, 48 h) possesses remarkable cell growth inhibitory activity toward HeLa, A549, HCT116, and MCF-7 cells, which are greater or similar with ZK304709^[1].
CDK9-IN-40 (1 μM-4 μM, 24 h) can cause the G2/M phase arrest and induce cell apoptosis in HCT116 cells in a concentration-dependent manner^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HeLa, A549, HCT116, MCF-7, HEK293, LO2
Concentration:

1 μM
Incubation Time:

48 h
Result:

Offered the best CDK9 inhibitory activities (IC₅₀ = 5.5 nM), being comparable to that of ZK304709 (IC₅₀ = 5.0 nM) and higher than AZD5438 (IC₅₀ = 18.0 nM).
Didn’t demonstrate obvious cytotoxic activity against two non-tumoural cells HEK-293 and LO2 (IC₅₀ = 50 μM).

Cell Cycle Analysis^[1]

Cell Line:

HCT116
Concentration:

1.0 μM, 2.0 μM, 4.0 μM
Incubation Time:

24 h
Result:

Induced a dose-dependent G2/M phase arrest (14.71%, 18.16%, and 24.81% respectively).

Apoptosis Analysis^[1]

Cell Line:

HCT116
Concentration:

1.0 μM, 2.0 μM, 4.0 μM
Incubation Time:

24 h
Result:

Induced total apoptosis rates of 10.08%, 16.43%, and 33.70% with the rate of 1.0, 2.0 and 4.0 μM, respectively.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	MRT_0-t	MRT_0-∞	AUC_0-t	AUC_0-∞	CL	V_z	C_max	F
Rat^[1]	1 mg/kg	i.v.	6.5 h	0.083 h	5.4 h	8.4 h	26.5 ng·h/mL	33.1 ng·h/mL	51.9 L/h/kg	375.3 L/kg	15.9 ng/mL	/
Rat^[1]	10 mg/kg	p.o.	3.6 h	4.0 h	125.2 h	155.8 h	6.9 ng·h/mL	7.9 ng·h/mL	117.2 L/h/kg	628.7 L/kg	18.6 ng/mL	41.7 %

体内実験

CDK9-IN-40 (Compound 8e) (60 mg/kg, PO, once daily, for 7 days) exhibits potent in vivo antitumor activity in HCT116 xenograft mouse models with tumor growth inhibition of 59.2%^[1].

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

Animal Model:

Four-week-old pathogen-free male Balb/c-nu mice were used to establish HCT116 xenograft models ^[1]
Dosage:

30 mg/kg, 60 mg/kg
Administration:

Oral gavage (PO); Once daily; for 7 days; 4 days after cell injection
Result:

Exhibited potent antitumor effects, suppressing tumor growth by 59.2% at a dose of 60 mg/kg per day.

化学情報

分子量 422.55
分子式 C₂₁H₂₆N₈S
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC(N4CCC5=C(SC(N)=N5)C4)=CC=N3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (270 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Chen L et al. Discovery and optimization of novel tetrahydrothiazolopyridine-based pyrimidines as highly potent cyclin-dependent kinase 9 (CDK9) inhibitors. Eur J Med Chem. 2025 Jun 14;296:117875. doi: 10.1016. https://pubmed.ncbi.nlm.nih.gov/40544651/

[2]. Chen L et al. Discovery and optimization of novel tetrahydrothiazolopyridine-based pyrimidines as highly potent cyclin-dependent kinase 9 (CDK9) inhibitors. Eur J Med Chem. 2025 Jun 14;296:117875. doi: 10.1016. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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CDK9-IN-40

CDK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

CDK9-IN-40 関連分類

HY-176736 関連分類