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
5 mg USD 108 In-stock
10 mg USD 180 In-stock
50 mg USD 648 In-stock
100 mg USD 1140 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of CFI-400945 free base:

  • 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

Ki: 0.26 nM (PLK4)[1]
IC50: 2.8 nM (PLK4)[1]

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].

References
Preparing Stock Solutions
Concentration Volume 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.
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]

CFI-400945 is prepared as 10 mM stocks in 100% DMSO and diluted with DMEM cell growth medium containing 10% FBS.

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]

CFI-400945 is dissolved in water.

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

Solvent & Solubility

DMSO: ≥ 166.66 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.45%

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