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

(1E)-CFI-400437 dihydrochloride 

Cat. No.: HY-132135
Handling Instructions

(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
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Estimated Time of Arrival: December 31
25 mg USD 650 In-stock
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50 mg USD 990 In-stock
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100 mg USD 1450 In-stock
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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]

PLK3

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (22.10 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
(1E)-CFI-400437 dihydrochloride
Cat. No.:
HY-132135
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