2. Cell Cycle/DNA Damage Cytoskeleton
  3. Mps1
  4. TTK-IN-5

TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer.

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

TTK-IN-5

TTK-IN-5 Chemical Structure

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TTK-IN-5 Related Antibodies

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Description

TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer[1].

In Vitro

TTK-IN-5 (Compound 19) (1 μM) displays potent and highly selective inhibitory activity against threonine tyrosine kinase (TTK), with an inhibition rate of 98.99% (IC50 = 8.918 nM)[1].
TTK-IN-5 (5 μM, 12 h) forms potent interactions with TTK and bound tightly with TTK[1].

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

TTK-IN-5 Related Antibodies
Parmacokinetics
Species Dose Route F T1/2 Tmax MRT0-t MRT0-∞ Cmax AUC0-t AUC0-∞ Vss CL C0
Mice 10 mg/kg p.o. 26.2 % 1.42 h 0.08 h 0.68 h 0.68 h 449.7 ng/mL 223 ng·h/mL 226 ng·h/mL / / /
Mice 2 mg/kg i.v. / 0.39 h 0.08 h 0.12 h 0.13 h 610 ng/mL 171 ng·h/mL 171 ng·h/mL 1.57 L/kg 194.6 mL/min/kg 1399 ng/mL
In Vivo

TTK-IN-5 (Compound 19) (7.5, 15 mg/kg, i.v., twice a week for 21 days) strongly suppresses tumor growth with low toxicity in the MDA-MB-231 xenograft mouse model[1].
TTK-IN-5 (30 mg/kg, p.o., once daily for 21 days) inhibits tumor growth in the A2780 xenograft mouse model[1].

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

Animal Model: MDA-MB-231 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
Dosage: 7.5, 15 mg/kg, Paclitaxel (HY-B0015) 10 mg/kg
Administration: Intravenous injection (i.v.), twice a week for 21 days
Result: Showed tumor growth inhibition (TGI) values of 49.3% and 66.0% at doses of 7.5 mg/kg and 15 mg/kg, respectively.
Markedly suppressed tumor growth (TGI = 75.0%), with no significant changes in animal body weights following combination treatment of Paclitaxel.
Inhibited tumor cell proliferation and markedly induced cell death when co-administrated with Paclitaxel.
Decreased phosphorylation of TTK in a dose dependent manner.
Increased Bax protein levels and suppressed Bcl-2 protein, explaining its apoptotic potency.
Animal Model: A2780 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
Dosage: 30 mg/kg
Administration: oral administration (p.o.), once daily for 21 days
Result: Effectively inhibited tumor growth, reaching the tumor growth inhibition (TGI) of 36.46%.
Significantly inhibited tumor volume.
Induced no significant changes in body weight.
Molecular Weight

533.53

Formula

C28H25F2N5O4
SMILES

COC1=CC=C(OC2=NC3=C(C4=CC(C)=C(C(NC5CC5)=O)C=C4)C=NN3C(N(C(C=C)=O)C)=C2)C(F)=C1F
Shipping

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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TTK-IN-5 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:

TTK-IN-5Mps1Monopolar spindle 1Threonine tyrosine kinase (TTK)Kinase inhibitorA2780MDA-MB-231covalentcancerInhibitorinhibitorinhibit

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