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.
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- 화학식: C28H25F2N5O4
- 분자량:533.53
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
| 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 |
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.
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Animal Model:MDA-MB-231 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
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Dosage:7.5, 15 mg/kg, Paclitaxel (HY-B0015) 10 mg/kg
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Administration:Intravenous injection (i.v.), twice a week for 21 days
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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.
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Animal Model:A2780 xenograft mouse model in female BALB/c nude mice (6-8 weeks)[1]
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Dosage:30 mg/kg
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Administration:oral administration (p.o.), once daily for 21 days
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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.
Chemical Information
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분자량 533.53
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화학식 C28H25F2N5O4
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TTK-IN-5 Related Classifications
HY-179430 Related Classifications
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