Art. -Nr.: HY-X0009

Tambiciclib

(Synonyms: GFH009; JSH-009; SLS009)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC₅₀ = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research.

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Reinheit: 99.68%
CAS. Nr.: 2247481-08-7
Formel: C₂₅H₃₅ClN₆O₂S
Molecular Weight:519.10

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Tambiciclib Chemical Structure

CAS. Nr.: 2247481-08-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK9

1 nM (IC₅₀)

Cdk1/cyclin B

5410 nM (IC₅₀)

cdk2/cyclin A

6850 nM (IC₅₀)

CDK3/cyclin E1

>10000 nM (IC₅₀)

Cdk5/p25

6950 nM (IC₅₀)

CDK7/Cyclin H/MNAT1

3700 nM (IC₅₀)

CDK8/cyclin C

>10000 nM (IC₅₀)

CDK11

>10000 nM (IC₅₀)

CDK14/Cyclin Y

2710 nM (IC₅₀)

CDK16/Cyclin Y

195 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle DYRK Isoform-spezifische Produkte anzeigen :

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Alle PARP Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	GI₅₀	0.014 μM Compound: 41	Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo assay	[PMID: 30253346]

In Vitro

Tambiciclib (JSH009) (72 h) potently inhibits the growth of diverse AML cell lines and patient-derived primary cells (GI₅₀ < 50 nM), but is far less potent against normal peripheral blood mononuclear cells (PBMCs) (GI₅₀ > 10 μM), supporting a favorable safety profile^[1].
Tambiciclib (0.03-3 μM, 2 h) potently and dose-dependently inhibits the phosphorylation of RNA Pol II at Ser2 (EC₅₀ < 300 nM) in OCI-AML-3, MV4-11, and HL-60 cells, while showing no effect on the CDK7-mediated phosphorylation of RNA Pol II at Ser5 or CDK9 at Thr186, confirming its high selectivity over CDK7^[1].
Tambiciclib (0.03-0.1 μM, 10 h) downregulates MCL1 and MYC expression at the transcriptional level alongside a broader reduction in overall transcription in MV4-11 cells^[1].
Tambiciclib (0.01-0.1 μM, 24 h) induces apoptosis in OCI-AML-3, MV4-11, and HL-60 cell lines, as evidenced by the cleavage of caspase-3 and PARP^[1].
Tambiciclib (0.01-0.05 μM, 24 h) has no effect on the cell cycle distribution of MV4-11 and OCI-AML-3 cells, consistent with the lack of significant changes in the expression of key cell cycle regulators (E2F1, Cyclin D1, CDC2) in MV4-11 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

OCI-AML-3, MV4-11, and HL-60 cells
Concentration:

0.03, 0.1, 0.3, 1, and 3 μM
Incubation Time:

2 h
Result:

Reduced p-RNA Pol II Ser2 and levels in a dose-dependent manner.
Did not affect the phosphorylation levels of RNA Pol II Ser5 or CDK9 Thr186, which are controlled by CDK7, even at a concentration of 3 μM.
Reduced MCL-1 and C-MYC protein levels.

Real Time qPCR^[1]

Cell Line:

MV4-11 cells
Concentration:

0.03 and 0.1 μM
Incubation Time:

10 h
Result:

Decreased MYC and MCL1 mRNA levels in MV4-11 cells.

Western Blot Analysis^[1]

Cell Line:

OCI-AML3, MV4-11, and HL-60 cells
Concentration:

0.01, 0.03, and 0.1 μM
Incubation Time:

24 h
Result:

Increased cleaved-caspase3 and cleaved-PARP levels in all three cell lines.
Elicited a markedly weaker PARP cleavage signal in OCI-AML3 cells compared to MV4-11 and HL-60 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	MRT_0-∞	F
Rat^[1]	1 mg/kg	i.v.	4.303 h	0.033 h	167.7 ng/mL	76.3 ng·h/mL	81.9 ng·h/mL	73437 mL/kg	12335 mL/h/kg	3.227 h	/
Rat^[1]	20 mg/kg	p.o.	2.313 h	4.000 h	119.7 ng/mL	681 ng·h/mL	770 ng·h/mL	89877 mL/kg	27431 mL/h/kg	7.45 h	47 %

In Vivo

Tambiciclib (10 and 20 mg/kg, P.O., daily for 3 weeks) inhibits tumor growth and exerts no obvious toxicity in the MV4-11 cell-inoculated xenograft mouse model^[1].
Tambiciclib (10 and 15 mg/kg, P.O., daily until endpoint) dose-dependently prolongs overall survival in the MV4-11 cell-derived engraftment mouse model^[1].
Tambiciclib (10 and 20 mg/kg, P.O., daily for approximately 2 weeks) displays dose-dependent efficacy against antitumor progression in an AML patient-derived xenograft (PDX) mouse model^[1].

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

Animal Model:

Female NOD-SCID mice (5 weeks old) intravenously injected with MV4-11 cells^[1]
Dosage:

10 and 15 mg/kg
Administration:

p.o., daily until endpoint
Result:

Prolonged overall survival in a dose-dependent manner.
Achieved almost 200 days of survival in mice at 15 mg/kg.

Animal Model:

Balb/c nu mice subcutaneously injected with MV4-11 cells^[1]
Dosage:

10 and 20 mg/kg
Administration:

p.o., daily for 3 weeks
Result:

Inhibited tumor growth with TGI of 25.2% at 10 mg/kg.
Almost completely suppressed tumor progression (TGI = 98.7%) at a 20 mg/kg dosage.
Revealed no apparent behavioral changes or body weight loss in mice.
Suppressed proliferation (Ki67) and induced apoptosis in a dose dependent manner.

Animal Model:

Female NCG mice (5 weeks old) subcutaneously implanted with AML patient tumors^[1]
Dosage:

10 and 20 mg/kg
Administration:

p.o., daily for approximately 2 weeks
Result:

Resulted in a TGI of 53.4% without any apparent overall toxicity at 20 mg/kg.
Displayed dose-dependent efficacy against antitumor progression.
Downregulated the phosphorylation of RNA Pol II and Mcl1/MYC protein levels.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2247481-08-7
Appearance Solid
Molecular Weight 519.10
Formel C₂₅H₃₅ClN₆O₂S
Color White to yellow
SMILES

COC[C@@H](C)N[C@@H](CC1)CC[C@H]1NC2=CC(C3=CSC(NCC4(CCOCC4)C#N)=N3)=C(Cl)C=N2
Synonyms

GFH009; JSH-009; SLS009
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Acta Pharm Sin B

Predicting and overcoming resistance to CDK9 inhibitors for cancer therapy. [Abstract]

2023 Sep;13(9):3694-3707. PMID: 37719386

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (192.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9264 mL

9.6321 mL

19.2641 mL

5 mM

0.3853 mL

1.9264 mL

3.8528 mL

10 mM

0.1926 mL

0.9632 mL

1.9264 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[1]. Wang L, et al. Discovery of a novel and highly selective CDK9 kinase inhibitor (JSH-009) with potent antitumor efficacy in preclinical acute myeloid leukemia models. Invest New Drugs. 2020 Oct;38(5):1272-1281. [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9264 mL	9.6321 mL	19.2641 mL	48.1603 mL
	5 mM	0.3853 mL	1.9264 mL	3.8528 mL	9.6321 mL
	10 mM	0.1926 mL	0.9632 mL	1.9264 mL	4.8160 mL
	15 mM	0.1284 mL	0.6421 mL	1.2843 mL	3.2107 mL
	20 mM	0.0963 mL	0.4816 mL	0.9632 mL	2.4080 mL
	25 mM	0.0771 mL	0.3853 mL	0.7706 mL	1.9264 mL
	30 mM	0.0642 mL	0.3211 mL	0.6421 mL	1.6053 mL
	40 mM	0.0482 mL	0.2408 mL	0.4816 mL	1.2040 mL
	50 mM	0.0385 mL	0.1926 mL	0.3853 mL	0.9632 mL
	60 mM	0.0321 mL	0.1605 mL	0.3211 mL	0.8027 mL
	80 mM	0.0241 mL	0.1204 mL	0.2408 mL	0.6020 mL
	100 mM	0.0193 mL	0.0963 mL	0.1926 mL	0.4816 mL

Tambiciclib

1 Cited Publications

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Tambiciclib

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Publications Citing Use of MedChemExpress (MCE) Tambiciclib

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DYRK Isoform-spezifische Produkte anzeigen

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Alle PARP Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tambiciclib Related Classifications

HY-X0009 Related Classifications