PD0325901

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MEK inhibitor

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Catalog No. A10256

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
PD0325901 5mg A10256-5

Regular Price: $45.00

Special Price: $38.25

PD0325901 10mg A10256-10

Regular Price: $90.00

Special Price: $76.50

PD0325901 25mg A10256-25

Regular Price: $150.00

Special Price: $127.50

PD0325901 100mg A10256-100

Regular Price: $360.00

Special Price: $306.00

PD0325901 10mM * 1mL in DMSO A10256-10mM-D

Regular Price: $107.00

Special Price: $90.95

Products are for laboratory research use only. Not for human use. We do not sell to patients.

Quick Overview

PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.

PD0325901

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Chemical Information

Catalog Num A10256
Actions Inhibitor
M. Wt 482.2
Formula C16H14F3IN2O4
Solubility DMSO>96mg/mL Water<1mg/mL Ethanol>96mg/mL
Purity >98%
Storage at -20°C 2 years
CAS No. 391210-10-9
Synonyms N/A
SMILES code C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOC[[email protected]@H](CO)O
Chemical Name N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide

Biological Activity

Description
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
Targets
MEK (Cell-free assay)
0.33 nM

Solubility

Solubility (25°C)* In vitro DMSO 96 mg/mL (199.09 mM)
Water <1 mg/mL (<1 mM)
Ethanol 40 mg/mL (82.95 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Biological Activity

Phase II clinical trials was published in 2010. The study propose was to evaluate the efficacy of mitogen-activated protein kinase/extracellular signal-related kinase kinase inhibitor PD0325901 in advanced non–small cell lung cancer patients who had experienced treatment failure after, or were refractory to, standard systemic therapy.  All patients had received prior systemic therapy (median of two regimens, including epidermal growth factor receptor inhibitors in 26%). Of 13 patients treated on schedule A, three discontinued due to adverse events (blurred vision, fatigue, and hallucinations, respectively). Twenty-one patients received schedule B. Main toxicities included diarrhea, fatigue, rash, vomiting, nausea, and reversible visual disturbances. Hematologic toxicity consisted mainly of mild-to-moderate anemia, without neutropenia. Chemistry abnormalities were rare. Mean (coefficient of variation) PD0325901 trough plasma concentrations were 100 ng/mL (52%) and 173 ng/mL (73%) for schedules A and B, respectively, above the minimum target concentration established in preclinical studies (16.5 ng/mL). There were no objective responses. Seven patients had stable disease. Median (95% confidence interval) progression-free survival was 1.8 months (1.5-1.9) and overall survival was 7.8 months (4.5-13.9). Conclusions: PD0325901 did not meet its primary efficacy end point. Future studies should focus on PD-0325901 schedule, rational combination strategies, and enrichment of patient selection based on mode of action.

Reference

1. Haura, Eric B.; Ricart, Alejandro D.; Larson, Timothy G.; Stella, Philip J.; Bazhenova, Lyudmila; Miller, Vincent A.; Cohen, Roger B.; Eisenberg, Peter D.; Selaru, Paulina; Wilner, Keith D.; Gadgeel, Shirish M. A Phase II Study of PD-0325901, an Oral MEK Inhibitor, in Previously Treated Patients with Advanced Non-Small Cell Lung Cancer. Clinical Cancer Research (2010), 16(8), 2450-2457. CODEN: CCREF4 ISSN:1078-0432. AN 2010:470634

2. Gaspar, Nathalie; Sharp, Swee Y.; Eccles, Suzanne A.; Gowan, Sharon; Popov, Sergey; Jones, Chris; Pearson, Andrew; Vassal, Gilles; Workman, Paul. Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma. Molecular Cancer Therapeutics (2010), 9(5), 1219-1233. CODEN: MCTOCF ISSN:1535-7163. AN 2010:573734 


3. Lo Russo, Patricia M.; Krishnamurthi, Smitha S.; Rinehart, John J.; Nabell, Lisle M.; Malburg, Lisa; Chapman, Paul B.; De Primo, Samuel E.; Bentivegna, Steven; Wilner, Keith D.; Tan, Weiwei; Ricart, Alejandro D. Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral MAPK/ERK Kinase Inhibitor PD-0325901 in Patients with Advanced Cancers. Clinical Cancer Research (2010), 16(6), 1924-1937. CODEN: CCREF4 ISSN:1078-0432. AN 2010:318287 

4. Wang, Yaolin; Wang, Yan; Liu, Ming; Bishop, Walter Robert; Seidel-Dugan, Cynthia. Anti-IGF-1 receptor antibody combined with chemotherapeutic agent, antitumor agent, radiotherapy or surgery for treating or preventing colorectal cancer. PCT Int. Appl. (2009), 52pp. CODEN: PIXXD2 WO 2009142810 A2 20091126 CAN 151:569615 AN 2009:1470605 

5. Mann, David Marshall. Gene expression profiling in the pulmonary artery in the selection of therapies for vascular-related diseases. PCT Int. Appl. (2009), 115pp. CODEN: PIXXD2 WO 2009121031 A1 20091001 CAN 151:418165 AN 2009:1194632 

6. Ohta, Yoshikazu; Takagi, Shinji; Yaguchi, Masahiro. Concomitant drug for treating cancer. PCT Int. Appl. (2009), 57pp. CODEN: PIXXD2 WO 2009110416 A1 20090911 CAN 151:328871 AN 2009:1107826 

7. Belvin, Marcia; Friedman, Lori; Hoeflich, Klaus; Sampath, Deepak; Vijapurkar, Ulka; Wallin, Jeffrey; Johnson, Leisa; Singh, Mallika; Patel, Sonal. Preparation of thienopyrimidinylmorpholine derivatives for use as phosphoinositide 3-kinase inhibitors. PCT Int. Appl. (2009), 189pp. CODEN: PIXXD2 WO 2009036082 A2 20090319 CAN 150:329836 AN 2009:333658 

8. Geroni, Maria Cristina; Valota, Olga; Ballinari, Dario; Marsiglio, Aurelio. A morpholinyl anthracycline derivative combined with protein kinase inhibitors for treatment of tumors. PCT Int. Appl. (2009), 14pp. CODEN: PIXXD2 WO 2009016072 A2 20090205 CAN 150:183373 AN 2009:139918 

9. Miner, Jeffrey N.; Chapman, Mark S.; Quart, Barry; Adjei, Alex; Yu, Chunrong. Combinations of MEK inhibitors and Raf kinase inhibitors and uses thereof. PCT Int. Appl. (2009), 148 pp. CODEN: PIXXD2 WO 2009018238 A1 20090205 CAN 150:191158 AN 2009:139541 

10. Wang, Yan; Pachter, Jonathan A.; Hailey, Judith Anne; Brams, Peter; Williams, Denise; Srinivasan, Mohan; Feingersh, Mary Diane. Anti-insulin-like growth factor 1 receptor therapy. PCT Int. Appl. (2009), 129pp. CODEN: PIXXD2 WO 2009005673 A1 20090108 CAN 150:119716 AN 2009:25215 

11. Tecle, Haile; Shao, Jianxing; Li, Yanhong; Kothe, Michael; Kazmirski, Steven; Penzotti, Julie; Ding, Yuan-Hua; Ohren, Jeffrey; Moshinsky, Deb; Coli, Rocco; Jhawar, Nidhi; Bora, Emilia; Jacques-O'Hagan, Suzanne; Wu, Joe. Beyond the MEK-pocket: Can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK? Bioorganic & Medicinal Chemistry Letters (2009), 19(1), 226-229. CODEN: BMCLE8 ISSN:0960-894X. CAN 150:251898 AN 2009:5970 

12. Barrett, Stephen D.; Bridges, Alexander J.; Dudley, David T.; Saltiel, Alan R.; Fergus, James H.; Flamme, Cathlin M.; Delaney, Amy M.; Kaufman, Michael; LePage, Sophie; Leopold, Wilbur R.; Przybranowski, Sally A.; Sebolt-Leopold, Judith; Van Becelaere, Keri; Doherty, Annette M.; Kennedy, Robert M.; Marston, Dan; Howard, W. Allen, Jr.; Smith, Yvonne; Warmus, Joseph S.; Tecle, Haile. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorganic & Medicinal Chemistry Letters (2008), 18(24), 6501-6504. CODEN: BMCLE8 ISSN:0960-894X. CAN 150:121301 AN 2008:1410214 

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