2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. (1E)-CFI-400437 dihydrochloride

(1E)-CFI-400437 dihydrochloride 

Cat. No.: HY-132135 Purity: 98.03%
COA Handling Instructions

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(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.

For research use only. We do not sell to patients.

(1E)-CFI-400437 dihydrochloride Chemical Structure

(1E)-CFI-400437 dihydrochloride Chemical Structure

CAS No. : 1247000-76-5

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5 mg USD 210 In-stock
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Based on 1 publication(s) in Google Scholar

(1E)-CFI-400437 dihydrochloride Related Antibodies

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Description

(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[1].

IC50 & Target[1]

PLK4

0.6 nM (IC50)

In Vivo

(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.
Molecular Weight

565.49

Formula

C29H30Cl2N6O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

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
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.

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  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
Purity & Documentation

Purity: 98.08%

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

Handling Instructions (2659 KB)
References

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.

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.

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(1E)-CFI-400437 dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(1E)-CFI-4004371247000-76-5Polo-like Kinase (PLK)PLK4anticancerantiproliferativeMCF-7MDA-MB-468MDA-MB-231cellsInhibitorinhibitorinhibit

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