1. TGF-beta/Smad
  2. TGF-β Receptor
  3. PF-06952229

PF-06952229 

Cat. No.: HY-136244 Purity: 99.70%
Handling Instructions

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer.

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

PF-06952229 Chemical Structure

PF-06952229 Chemical Structure

CAS No. : 1801333-55-0

Size Price Stock Quantity
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 700 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction. PF-06952229 is a promising antineoplastic agent for the study solid tumors, especifically metastatic breast cancer[1].

IC50 & Target

IC50: transforming growth factor-beta receptor 1 (TGFbR1)[1]

In Vivo

PF-06952229 (oral gavage; 30 mg/kg; twice daily; 21 days) combines with Palbociclib 21 days results in an improved inhibition of pSMAD2 in the MCF7 ER+ xenograft breast cancer tumor model. This combination also leads to a significant increase in survival relative to PF-06952229 monotherapy[1].

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

Animal Model: MCF-7 ER+ HER2-xenograft breast cancer tumor model[1]
Dosage: 30 mg/kg
Administration: Oral gavage; twice daily; 44 days
Result: Resulted in an increase in tumor growth inhibition when combined with Palbociclib.
Clinical Trial
Molecular Weight

458.91

Formula

C₂₃H₂₄ClFN₄O₃

CAS No.

1801333-55-0

SMILES

O=C(NC(CO)CO)C1=CN=CC=C1NC2=CC(C3=CC(Cl)=CC=C3F)=NC=C2C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (181.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1791 mL 10.8954 mL 21.7908 mL
5 mM 0.4358 mL 2.1791 mL 4.3582 mL
10 mM 0.2179 mL 1.0895 mL 2.1791 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-06952229PF06952229PF 06952229TGF-β ReceptorTransforming growth factor beta receptorsbreastcancerCT26cellsMCF-7SolidtumorsMetastaticdifferentiationapoptosismotilityinvasionangiogenesisInhibitorinhibitorinhibit

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Product Name:
PF-06952229
Cat. No.:
HY-136244
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