Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vivo |
In the MCF7 ER+ xenograft breast cancer tumor model, PF-06952229 (oral gavage; 30 mg/kg; twice daily; 21 days) paired with palbociclib for 21 days increases pSMAD2 suppression. Comparing this combination to PF-06952229 monotherapy, survival was likewise markedly increased [1].
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Animal Protocol |
Animal/Disease Models: MCF-7 ER+ HER2-xenograft breast cancer tumor model [1]
Doses: 30 mg/kg Route of Administration: po (oral gavage); twice (two times) daily; 44 days Experimental Results: Tumor growth inhibition when combined with Palbociclib Enhance. |
References | |
Additional Infomation |
TGF-beta Receptor 1 Inhibitor PF-06952229 is an orally bioavailable inhibitor of transforming growth factor-beta receptor 1 (TGFbR1), with potential antineoplastic activity. Upon administration, TGF-betaR1 inhibitor PF-06952229 specifically targets and binds to TGFbR1, which prevents TGFbR1-mediated signal transduction. This abrogates TGFbR1-mediated immunosuppression, enhances anti-tumor immunity in the tumor microenvironment (TME) and promotes a cytotoxic T-lymphocyte (CTL)-mediated immune response against tumor cells leading to tumor cell death. This may lead to a reduction in TGFbR1-dependent proliferation of cancer cells. The TGFb signaling pathway is often deregulated in tumors and plays a key role in the regulation of cell growth, differentiation, apoptosis, motility, invasion, and angiogenesis. It plays a key role in immunosuppression in the TME.
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Molecular Formula |
C23H24CLFN4O3
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Molecular Weight |
458.913067817688
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Exact Mass |
458.152
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CAS # |
1801333-55-0
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PubChem CID |
118211239
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Appearance |
White to off-white solid powder
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LogP |
3.4
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Hydrogen Bond Donor Count |
4
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Hydrogen Bond Acceptor Count |
7
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Rotatable Bond Count |
8
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Heavy Atom Count |
32
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Complexity |
598
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Defined Atom Stereocenter Count |
0
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SMILES |
ClC1=CC=C(C(=C1)C1=CC(=C(C=N1)C(C)C)NC1C=CN=CC=1C(NC(CO)CO)=O)F
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InChi Key |
IPBLCOKXDQHSQW-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H24ClFN4O3/c1-13(2)17-10-27-21(16-7-14(24)3-4-19(16)25)8-22(17)29-20-5-6-26-9-18(20)23(32)28-15(11-30)12-31/h3-10,13,15,30-31H,11-12H2,1-2H3,(H,28,32)(H,26,27,29)
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Chemical Name |
4-[[2-(5-chloro-2-fluorophenyl)-5-propan-2-ylpyridin-4-yl]amino]-N-(1,3-dihydroxypropan-2-yl)pyridine-3-carboxamide
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Synonyms |
PF06952229 PF 06952229
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~50 mg/mL (~108.95 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.