2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. TSL2109

TSL2109 is an orally active and selective DYRK2 and CDK4/6 inhibitor with an IC50 value of 22 nM for DYRK2. TSL2109 exhibits high kinase selectivity over 93%. TSL2109 arrests cell cycle and induces apoptosis in virto. TSL2109 effectively overcomes Enzalutamide (HY-70002) resistance by suppressing tumor growth in vivo and virto. TSL2109 also shows CDK4/6 inhibitor resistance.TSL2109 demonstrates safety profile. TSL2109 can be used for prostate cancer research and breast cancer[1][2].

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TSL2109

TSL2109 Chemical Structure

CAS No. : 2619847-12-8

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TSL2109 Related Antibodies

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DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

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Description

TSL2109 is an orally active and selective DYRK2 and CDK4/6 inhibitor with an IC50 value of 22 nM for DYRK2. TSL2109 exhibits high kinase selectivity over 93%. TSL2109 arrests cell cycle and induces apoptosis in virto. TSL2109 effectively overcomes Enzalutamide (HY-70002) resistance by suppressing tumor growth in vivo and virto. TSL2109 also shows CDK4/6 inhibitor resistance.TSL2109 demonstrates safety profile. TSL2109 can be used for prostate cancer research and breast cancer[1][2].
In Vitro

TSL2109 (0.5-2 μM,72 h-5 days) exhibits potent antiproliferative activity (IC50 = 0.933 μM) and dose-dependent cell growth inhibitory activity in PCa DU145 cells and exerts significant inhibitory effects proliferation, induces significant G1 phase cell cycle arrest, and promotes apoptosis in 22Rv1 cell [1].
TSL2109 (0.5-2 μM, 24 h) arrests cell cycle at G1 phase and promotes apoptosis in DU145 cells[1].
TSL2109 significantly inhibits the E2F targets and G2M checkpoint pathways in DU145 cells and 22Rv1 cells , upregulates the apoptosis and P53 pathways in DU145 cells[1].
TSL2109 (0.001-1000 μM, 7 days) demonstrates superior growth inhibition in Enzalutamide-resistant in PCa organoids (PDOs) (PR6513B) [1].
TSL2109 significantly suppresses proliferation in androgen receptor (AR) inhibitor-resistant PCa cells and organoids[2].
TSL2109 downregulates p-RB, p-4E-BP1 and BCL2[2].
TSL2109 markedly suppresses the E2F and G2M signaling pathways[2].

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

TSL2109 Related Antibodies

Cell Viability Assay[1]

Cell Line: PCa DU145 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 5 days
Result: Shows a dose-dependent cell growth inhibitory activity.

Cell Cycle Analysis[1]

Cell Line: DU145 and 22Rv1 cell cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Arrested cell cycle at G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: DU145 and 22Rv1 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Promoted apoptosis in a concentration-dependent manner.

Cell Proliferation Assay[1]

Cell Line: 22Rv1 and DU145 cell
Concentration: 0.5, 1, 2 μM
Incubation Time: 72 h
Result: Exerted significant inhibitory effects on 22Rv1 cell proliferation.
In Vivo

TSL2109 (100-200 mg/kg, o.p, once daily for 45 days) shows a favorable safety profile in DU145 mice xenografts[1].
TSL2109 (1000 mg/kg, o.p, once) has excellent tolerability and no adverse behavioral effects with safety profile in DU145 mice xenografts[1].
TSL2109 (75 mg/kg, o.p, once daily for 21 days) demonstrates the potential in overcoming Enzalutamide resistance and shows promise in enhancing the efficacy of enzalutamide[1].
TSL2109 (100 mg/kg, once a day for 30 days) demonstrates the potential in overcoming Enzalutamide in in Enzalutamide-resistant PDX mice models[1].
TSL2109 effectively inhibits tumor growth of AR inhibitor-resistant PDX models[2].
TSL2109 shows a potent efficacy in CDK4/6 inhibitor-resistant breast cancer models[2].

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

Animal Model: DU145 cell induced-Male BALB/c nude mice[1]
Dosage: 1000 mg/kg
Administration: o.p, once
Result: Exhibited normal body weight gain.
Caused no adverse behavioral effects during a 48 h observation period.
Maintained normal weight gain over 14 days.
Observed no significant changes in the weights of major organs (heart, liver, spleen, lung, kidney) after 14 days.
Animal Model: DU145 cell induced-Male BALB/c nude mice[1]
Dosage: 100 and 200 mg/kg
Administration: o.p, once daily for 15 days
Result: Obviously inhibited 22Rv1 xenografts tumor growth.
Improved tumor growth inhibitory activity when combination with Enzalutamide.
Animal Model: PDX tissue (s.c.) induced-male NU/ NU mice[1]
Dosage: 100 mg/kg
Administration: once a day for 30 days
Result: Induced robust tumor growth suppression.
Significantly reduced tumor burden.
Clinical Trial
Molecular Weight

548.68

Formula

C28H33FN8OS
CAS No.
SMILES

FC1=C(C2=CC=C3N=C(SC3=C2)N(CC)CC)N=C(NC4=NC=C(C=C4)C(N5CCN(CC5)C(C)C)=O)N=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TSL2109 Related Classifications

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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:

TSL21092619847-12-8TSL 2109TSL-2109DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseInhibitorinhibitorinhibit

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