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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1430741-35-7
分子式: C₃₀H₃₁N₅O₂
分子量:493.60

保管条件:

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

Data Sheet (277 KB)

CFI-401870 構造式

CAS 番号: 1430741-35-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示 :

体外実験

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 %

体内実験

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.

化学情報

CAS 番号 1430741-35-7
分子量 493.60
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (277 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

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分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Keywords

100 mg

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生物活性
- 製品説明
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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CFI-401870

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

CFI-401870 関連分類

HY-116190 関連分類