PF-06952229 - 99%, high purity , CAS No.1801333-55-0

  • ≥99%
Item Number
P649080
Grouped product items
SKUSizeAvailabilityPrice Qty
P649080-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$350.90
P649080-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$600.90
View related series
TGF-beta/Smad TGF-β Receptor

Basic Description

Synonyms1KKS7U3X86 | SCHEMBL16879380 | 3-Pyridinecarboxamide, 4-((2-(5-chloro-2-fluorophenyl)-5-(1-methylethyl)-4-pyridinyl)amino)-N-(2-hydroxy-1-(hydroxymethyl)ethyl)- | AKOS040734464 | PF06952229 | PF-06952229 | CS-0120989 | MS-28403 | PF 06952229 [WHO-DD] | BD
Specifications & Purity≥99%
Biochemical and Physiological MechanismsPF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.xa0PF-06952229 is a promising antineoplasticxa0agent for the study solid tumors, especifically
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product 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

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 . 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 Dosage: 30 mg/kg Administration: Oral gavage; twice daily; 44 days Result: Resulted in an increase in tumor growth inhibition when combined with Palbociclib.

Form:Solid

IC50& Target:IC50: transforming growth factor-beta receptor 1 (TGFbR1)

Associated Targets(Human)

TGFBR1 Tchem TGF-beta receptor type I (3786 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BMPR1A Tchem Bone morphogenetic protein receptor type-1A (678 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACVR1B Tchem Activin receptor type-1B (1131 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACVRL1 Tchem Serine/threonine-protein kinase receptor R3 (538 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BMPR1B Tchem Bone morphogenetic protein receptor type-1B (563 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACVR1 Tchem Activin receptor type-1 (1516 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

MC-38 (857 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
4T1 (1737 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CT26 (928 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[[2-(5-chloro-2-fluorophenyl)-5-propan-2-ylpyridin-4-yl]amino]-N-(1,3-dihydroxypropan-2-yl)pyridine-3-carboxamide
INCHI 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)
InChi Key IPBLCOKXDQHSQW-UHFFFAOYSA-N
Canonical SMILES CC(C)C1=CN=C(C=C1NC2=C(C=NC=C2)C(=O)NC(CO)CO)C3=C(C=CC(=C3)Cl)F
Isomeric SMILES CC(C)C1=CN=C(C=C1NC2=C(C=NC=C2)C(=O)NC(CO)CO)C3=C(C=CC(=C3)Cl)F
Alternate CAS 1801333-55-0
PubChem CID 118211239
Molecular Weight 458.91

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 50 mg/mL (108.95 mM; Need ultrasonic)

Related Documents

Solution Calculators