(1E)-CFI-400437 dihydrochloride

Name: (1E)-CFI-400437 dihydrochloride
Brand: MedChemExpress
SKU: HY-132135
Rating: 4.5 (1 reviews)

製品番号: HY-132135 純度: 98.03%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC₅₀= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC₅₀s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.

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(1E)-CFI-400437 dihydrochloride 構造式

CAS 番号 : 1247000-76-5

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 261	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 261	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$210	在庫あり	Estimated Time of Arrival: December 31
10 mg	$320	在庫あり	Estimated Time of Arrival: December 31
25 mg	$530	在庫あり	Estimated Time of Arrival: December 31
50 mg	$740	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1050	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Polo-like Kinase (PLK) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

PLK1 PLK2 PLK3 PLK4

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

PLK4

0.6 nM (IC₅₀)

体内実験

(1E)-CFI-400437 (25 mg/kg; intraperitoneal injection; daily for 21 days) dihydrochloride shows effective in a mouse xenograft model of tumor growth^[1].
The plasma levels of (1E)-CFI-400437 (50 mg/kg; IP; mice) dihydrochloride shows a Cmax of 92 ng/mL and AUC of 190 ng•h/mL, respectively. The mouse plasma protein binding measurement for (1E)-CFI-400437 is 99%, i.e., unbound compound in plasma is 1%^[1].

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

Animal Model:	6-8 week old female CB-17 SCID mice (MDA-MB-468 mouse xenograft model)^[1]
Dosage:	25 mg/kg
Administration:	Intraperitoneal injection; daily for 21 days
Result:	Effective in a mouse xenograft model of tumor growth. In this study, (1E)-CFI-400437 is weighed and suspended in PEG400:water (30:70) and sonicated at rt for 30 min. The compound is dispensed in aliquots and stored at −20 C° for the duration of the study, and each aliquot was thawed at room temperature before each dose.

分子量

565.49

分子式

C₂₉H₃₀Cl₂N₆O₂

CAS 番号

1247000-76-5

Appearance

Solid

Color

Brown to orange

SMILES

Cl[H].Cl[H].COC1=CC(/C2=C/C3=CC4=C(C(/C=C/C5=CC=C(N=C5)N6CCN(CC6)C)=NN4)C=C3)=C(C=C1)NC2=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度

体外:

DMSO : 12.5 mg/mL (22.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (1.77 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7684 mL	8.8419 mL	17.6838 mL
5 mM	0.3537 mL	1.7684 mL	3.5368 mL
10 mM	0.1768 mL	0.8842 mL	1.7684 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

純度: 98.08%

Select Batch:

データシート (278 KB) SDS (393 KB)

COA (257 KB) HNMR (308 KB) LCMS (105 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Laufer R, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013;56(15):6069-6087. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.7684 mL	8.8419 mL	17.6838 mL	44.2094 mL
DMSO	5 mM	0.3537 mL	1.7684 mL	3.5368 mL	8.8419 mL
	10 mM	0.1768 mL	0.8842 mL	1.7684 mL	4.4209 mL
	15 mM	0.1179 mL	0.5895 mL	1.1789 mL	2.9473 mL
	20 mM	0.0884 mL	0.4421 mL	0.8842 mL	2.2105 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.