2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Apoptosis Epigenetics
  3. CDK DYRK Apoptosis Bcl-2 Family c-Myc Caspase PARP DNA/RNA Synthesis
  4. Tambiciclib dimaleate

Tambiciclib dimaleate  (Synonyms: GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate)

Cat. No.: HY-X0009A Purity: 99.53%
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Tambiciclib (GFH009, JSH-009) dimaleate 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 dimaleate 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 dimaleate can be used for AML research.

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

Tambiciclib dimaleate

Tambiciclib dimaleate Chemical Structure

CAS No. : 2559759-04-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Tambiciclib dimaleate:

Tambiciclib dimaleate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tambiciclib dimaleate

View All CDK Isoform Specific Products:

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

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

View All DNA/RNA Synthesis Isoform Specific Products:

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tambiciclib (GFH009, JSH-009) dimaleate 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 dimaleate 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 dimaleate can be used for AML research[1].

IC50 & Target[1]

CDK9/cyclinT1

1 nM (IC50)

CDK1/cyclinB

5410 nM (IC50)

CDK2/cyclinA

6850 nM (IC50)

CDK3/cyclin E1

>10,000 nM (IC50)

Cdk5/p25

6950 nM (IC50)

CDK7/Cyclin H/MNAT1

3700 nM (IC50)

CDK8/cyclin C

>10,000 nM (IC50)

CDK11

>10,000 nM (IC50)

CDK14/Cyclin Y

2710 nM (IC50)

CDK16/Cyclin Y

195 nM (IC50)

In Vitro

Tambiciclib (JSH009) dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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 dimaleate (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.

Tambiciclib dimaleate Related Antibodies

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.

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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ Vz CL MRT0-∞ 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 dimaleate (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 dimaleate (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 dimaleate (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: 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 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: 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.
Molecular Weight

751.25

Formula

C33H43ClN6O10S
CAS No.
Appearance

Solid

Color

Off-white to light 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.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (133.11 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 1.3311 mL 6.6556 mL 13.3111 mL
5 mM 0.2662 mL 1.3311 mL 2.6622 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 (stored under nitrogen). 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

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (3.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    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: ≥ 2.5 mg/mL (3.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

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 (stored under nitrogen). 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 1.3311 mL 6.6556 mL 13.3111 mL 33.2779 mL
5 mM 0.2662 mL 1.3311 mL 2.6622 mL 6.6556 mL
10 mM 0.1331 mL 0.6656 mL 1.3311 mL 3.3278 mL
15 mM 0.0887 mL 0.4437 mL 0.8874 mL 2.2185 mL
20 mM 0.0666 mL 0.3328 mL 0.6656 mL 1.6639 mL
25 mM 0.0532 mL 0.2662 mL 0.5324 mL 1.3311 mL
30 mM 0.0444 mL 0.2219 mL 0.4437 mL 1.1093 mL
40 mM 0.0333 mL 0.1664 mL 0.3328 mL 0.8319 mL
50 mM 0.0266 mL 0.1331 mL 0.2662 mL 0.6656 mL
60 mM 0.0222 mL 0.1109 mL 0.2219 mL 0.5546 mL
80 mM 0.0166 mL 0.0832 mL 0.1664 mL 0.4160 mL
100 mM 0.0133 mL 0.0666 mL 0.1331 mL 0.3328 mL
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Tambiciclib dimaleate 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:

Tambiciclib dimaleate2559759-04-3GFH009 dimaleate JSH-009 dimaleate SLS009 dimaleateCDKDYRKApoptosisBcl-2 Familyc-MycCaspasePARPDNA/RNA SynthesisCyclin dependent kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseMycpoly ADP ribose polymeraseCDK9DYRK1A/BantileukemicAMLRNA Pol IIMCL1MYCapoptosisOCI-AML-3MV4-11HL-60Inhibitorinhibitorinhibit

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