1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)

CFI-400945 free base 

Cat. No.: HY-12300 Purity: 98.45%
Handling Instructions

CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.

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

CFI-400945 free base Chemical Structure

CFI-400945 free base Chemical Structure

CAS No. : 1338806-73-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 127 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of CFI-400945 free base:

View All Polo-like Kinase (PLK) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.

IC50 & Target[1]

PLK4

2.8 nM (IC50)

AURKA

140 nM (IC50)

AURKB/INCENP

98 nM (IC50)

TIE2/TEK

22 nM (IC50)

TRKA

6 nM (IC50)

TRKB

9 nM (IC50)

In Vitro

CFI-400945 (compound 48) shows potent inhibitory activities against a panel of kinases, including PLK4, TRKA, TRKB, AURKA, AURKB/INCENP, and TIE2/TEK, with IC50s of 2.8, 6, 9, 140, 98, 22 nM, and EC50s of 12, 84, 88, 510, 102, 117 nM, respectively. CFI-400945 exhibits growth inhibition effects on breast, lung, ovarian and colon cancer cells. The IC50s (in μM) are as follows: SKBr-3 (5.3), Cal-51 (0.26), BT-20 (0.058), A549 (0.005), OVCAR-3 (0.018), SW620 (0.38), Colo-205 (0.017), and HCT116+/+ (0.004) [1]. CFI-400945 inhibits autophosphorylation of PLK4 at serine 305 with an EC50 value of 12.3 nM in cells overexpressing PLK4. Cancer cells treated with CFI-400945 exhibit effects consistent with PLK4 kinase inhibition, including dysregulated centriole duplication, mitotic defects, and cell death[2].

In Vivo

Oral administration of CFI-400945 (3.0, 9.4 mg/kg) to mice bearing human cancer xenografts results in the significant inhibition of tumor growth at doses that are well tolerated. Increased antitumor activity is observed in PTEN-deficient compared to PTEN wild-type cancer xenografts. The maximum tolerated dose for once-daily administration of CFI-400945 is estimated to be 7.5-9.5 mg/kg[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 166.66 mg/mL (311.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8704 mL 9.3519 mL 18.7038 mL
5 mM 0.3741 mL 1.8704 mL 3.7408 mL
10 mM 0.1870 mL 0.9352 mL 1.8704 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

Active PLK4 is purified and used to measure PLK4 activity, using an indirect ELISA detection system. PLK1, PLK2, PLK3, AURKA, and AUKB/INCENP compound inhibition are determined using FRET-based homogeneous assay kits from Invitrogen. The assays are performed with ATP concentrations of 25, 60, and 80 μM, respectively, for PLK1, PLK2, and PLK3 and ATP concentrations of 20 and 128 μM, respectively, for AURKA and AURKB/INCENP[1].

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

Cell Assay
[2]

MDA-MB-468, MCF-7, HCC1954, MDA-MB-231, SKBr-3, Cal-51, and BT-20 breast cancer cells are treated with 10 nM to 50 μM CFI-400945 for 5 days. Cell viability is measured using SRB assay[2].

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

Animal Administration
[2]

To treat an established tumor, CFI-400945 and the vehicle (water) are administered by oral gavage (2.5-20 mg/kg), and 5-FU and carboplatin are administered by intraperitoneal injection to mice as described in the text. Animal weights are monitored daily, and tumor volume is measured three times per week[2].

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

References
Molecular Weight

534.65

Formula

C₃₃H₃₄N₄O₃

CAS No.

1338806-73-7

SMILES

O=C([[email protected]@]12[[email protected]](C3=CC4=C(C=C3)C(/C=C/C5=CC=C(CN6C[[email protected]@H](C)O[[email protected]@H](C)C6)C=C5)=NN4)C1)NC7=C2C=C(OC)C=C7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.45%

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CFI-400945 free base
Cat. No.:
HY-12300
Quantity:

CFI-400945 free base

Cat. No.: HY-12300