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

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

Cat. No.: HY-X0009 Purity: 99.21%
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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.

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

Tambiciclib

Tambiciclib Chemical Structure

CAS No. : 2247481-08-7

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

Other Forms of Tambiciclib:

Tambiciclib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Tambiciclib

View All CDK Isoform Specific Products:

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

View All DYRK Isoform Specific Products:

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

View All Bcl-2 Family Isoform Specific Products:

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

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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

View All PARP Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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)

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.

Tambiciclib Related Antibodies

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[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 4.303 h
Rat 20 mg/kg p.o. T1/2 2.313 h
Rat 1 mg/kg i.v. Tmax 0.033 h
Rat 20 mg/kg p.o. Tmax 4.000 h
Rat 1 mg/kg i.v. Cmax 167.7 ng/mL
Rat 20 mg/kg p.o. Cmax 119.7 ng/mL
Rat 1 mg/kg i.v. AUC0-t 76.3 ng·h/mL
Rat 20 mg/kg p.o. AUC0-t 681 ng·h/mL
Rat 1 mg/kg i.v. AUC0-∞ 81.9 ng·h/mL
Rat 20 mg/kg p.o. AUC0-∞ 770 ng·h/mL
Rat 1 mg/kg i.v. Vz 73437 mL/kg
Rat 20 mg/kg p.o. Vz 89877 mL/kg
Rat 1 mg/kg i.v. CL 12335 mL/h/kg
Rat 20 mg/kg p.o. CL 27431 mL/h/kg
Rat 1 mg/kg i.v. MRT0-∞ 3.227 h
Rat 20 mg/kg p.o. MRT0-∞ 7.45 h
Rat 20 mg/kg p.o. F 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
Molecular Weight

519.10

Formula

C25H35ClN6O2S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9264 mL 9.6321 mL 19.2641 mL
5 mM 0.3853 mL 1.9264 mL 3.8528 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 (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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.21%

SDS (252 KB)

COA (246 KB)

Handling Instructions (2659 KB)
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 (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.

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
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Tambiciclib 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:

Tambiciclib2247481-08-7GFH009 JSH-009 SLS009GFH 009GFH-009JSH009JSH 009JSH-009SLS009SLS 009SLS-009CDKDYRKApoptosisBcl-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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