PF-06952229 | CAS#1801333-55-0 | TGFbR1 inhibitor

MedKoo Cat#: 462426 | Name: PF-06952229

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

PF-06952229

CAS#1801333-55-0

Theoretical Analysis

MedKoo Cat#: 462426

Name: PF-06952229

CAS#: 1801333-55-0

Chemical Formula: C23H24ClFN4O3

Exact Mass: 458.1521

Molecular Weight: 458.92

Elemental Analysis: C, 60.20; H, 5.27; Cl, 7.72; F, 4.14; N, 12.21; O, 10.46

Price and Availability

Size	Price	Availability
5mg	USD 650.00	2 Weeks
10mg	USD 1,150.00	2 Weeks
50mg	USD 2,950.00	2 Weeks

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Related CAS #

No Data

Synonym

PF-06952229; PF-06952229; PF-06952229; MDV6058

IUPAC/Chemical Name

4-((2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-yl)amino)-N-(1,3-dihydroxypropan-2-yl)nicotinamide

InChi Key

IPBLCOKXDQHSQW-UHFFFAOYSA-N

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)

SMILES Code

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

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor.

In vitro activity:

TBD

In vivo activity:

TBD

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	50.0	108.95

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 458.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

TBD

In vitro protocol:

TBD

In vivo protocol:

TBD

1: Flavia Mercer Pernasetti, et al. Combinations of tgfb inhibitors and cdk inhibitors for the treatment of breast cancer. Patent WO2020058820A1. Pujala B, Ramachandran SA, Sonawane M, Kamble MM, Panpatil D, Adhikari S, Soni S, Subbareddy V, Shinde BU, Nayak AK, Bansal C, Gupta A, Mukherjee K, Agarwal AK, Guerrero J, Herrera FJ, Bernales S, Guha M, Chakravarty S, Pham SM, Rai R. Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization. Bioorg Med Chem Lett. 2022 Nov 1;75:128979. doi: 10.1016/j.bmcl.2022.128979. Epub 2022 Sep 8. PMID: 36089110. 2: Pujala B, Ramachandran SA, Sonawane M, Kamble MM, Panpatil D, Adhikari S, Soni S, Subbareddy V, Shinde BU, Nayak AK, Bansal C, Gupta A, Mukherjee K, Agarwal AK, Guerrero J, Herrera FJ, Bernales S, Guha M, Chakravarty S, Pham SM, Rai R. Discovery of MDV6058 (PF-06952229), a selective and potent TGFβR1 inhibitor: Design, synthesis and optimization. Bioorg Med Chem Lett. 2022 Nov 1;75:128979. doi: 10.1016/j.bmcl.2022.128979. Epub 2022 Sep 8. PMID: 36089110. 3: Guha M, Thibault S, Pham S, Bernales S, Pai R, Herrera FJ, Johnson TR, Vitsky A, Fernando T, Finkelstein M. Nonclinical Profile of PF-06952229 (MDV6058), a Novel TGFβRI/Activin Like Kinase 5 Inhibitor Supports Clinical Evaluation in Cancer. J Pharmacol Exp Ther. 2024 Oct 18;391(2):335-345. doi: 10.1124/jpet.124.002193. PMID: 39284628.