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Art. -Nr.: HY-116190

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CFI-401870

CFI-401870 is an orally active threonine tyrosine kinase (TTK (Mps1)) inhibitor with an IC₅₀ of 3.1 nM. CFI-401870 exhibits IC₅₀s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer.

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CAS. Nr.: 1430741-35-7
Formel: C₃₀H₃₁N₅O₂
Molecular Weight:493.60

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

CFI-401870 Chemical Structure

CAS. Nr.: 1430741-35-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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In Vitro

CFI-401870 inhibits MDA-MB-468, HCT-116 and OVCAR-3 cell proliferation with GI₅₀s of 36, 17 and 80 nM^[1].
CFI-401870 (0.05-3 μM, 48 h) induces G2/M phase arrest in a concentration-dependent manner, accompanied by a significant increase in the proportion of polyploid cells in HCT116 cells^[1].
CFI-401870 (0.1-0.5 μM, 6-28 h) leads to abnormal chromosome arrangement and defects in the spindle checkpoint in HCT116 cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

HCT116 cells
Concentration:

0.05, 0.1, 0.2, 0.5, 1 and 3 μM
Incubation Time:

48 h
Result:

Induced G2/M phase arrest in a concentration-dependent manner.

Parmacokinetics

Species	Dose	Route	C_max	AUC_inf	CL	T_1/2	F
Mice^[1]	10 mg/kg	p.o.	2 μg/mL	3 μg·h/mL	/	/	/
Rat^[1]	1 mg/kg	i.v.	/	0.25 μg·h/mL	66 mL/min/kg	0.78 h	/
Rat^[1]	5 mg/kg	p.o.	/	0.55 μg·h/mL	/	/	44 %

In Vivo

CFI-401870 (23-35 mg/kg, p.o., once daily for 21 days) demonstrates significant anti-tumor activity in multiple xenograft models of HCT116 colon cancer, MDA-MB-468 breast cancer and SW48 colon cancer in mice^[1].

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

Animal Model:

HCT116 colon cancer model established in female CD-1 nude mice^[1]
Dosage:

23 and 35 mg/kg
Administration:

Oral administration (p.o.), once daily for 21 days
Result:

Exhibited 77% and 55% tumor growth inhibition (TGI) for 75 at 35 and 23 mg/kg, respectively.

Chemical Information

CAS. Nr. 1430741-35-7
Molecular Weight 493.60
Formel C₃₀H₃₁N₅O₂
SMILES

O[C@@H]1C[C@H](CC[C@@H]2C1)N2C3=CC=C(C=C3)C4=NNC5=C4C=C(C=C5)C(N[C@H](C6CC6)C7=NC=CC=C7)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu Y, et al. The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents. J Med Chem. 2015 Apr 23;58(8):3366-92. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
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- In Vivo
Chemical Information
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CFI-401870

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CFI-401870 Related Classifications

HY-116190 Related Classifications