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Cat. No.: 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 No.: 1430741-35-7
Formule: C₃₀H₃₁N₅O₂
Masse moléculaire:493.60

Stockage:

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

Data Sheet (277 KB)

CFI-401870 Chemical Structure

CAS No.: 1430741-35-7

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Activité biologique
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

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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 No. 1430741-35-7
Masse moléculaire 493.60
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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]

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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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Activité biologique
- Description
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- In Vivo
Chemical Information
Pureté et documentation
Références

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CFI-401870

Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

CFI-401870 Related Classifications

HY-116190 Related Classifications