PD-325901, Free Base CAS 391210-10-9

CAS Number

391210-10-9

Grade

Highly Purified

Molecular Formula

C₁₆H₁₄F₃IN₂O₄

Molecular Weight

482.19

EU Commodity Code

38220090

UN DOT Shipping

UN 2811 PG III

Shipping Temp

Blue Ice

Storage Temp

-20°C

N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2[(2-fluoro-4-iodophenyl)amino]-benzamide; PD 0325901, MEK1/2 Inhibitor III

A selective and ATP non-competitive MEK inhibitor that suppresses the phosphorylation of ERK in murine colon 26 tumors (IC50 = 0.33nM). In combination with the GSK-3 inhibitor CHIR99021, prevents cell differentiation and sustains self-renewal of embryonic stem (ES) cells. PD 325901 is an inhibitor of mitogen activated protein kinase kinase (MEK or MAPKK). The potency, solubility and effectiveness of PD 325901 are greatly improved compared to PD 184352 (CI-1040).

PD 325901 potently inhibited the growth of melanoma cells, with and without BRAF mutation. It also had an antiangiogenic activity. The sensitivity of RAS mutant cancers to MEK inhibitors depends on the activity of the phosphatidylinositol 3-kinase (PI3K) pathway.

The antiproliferative effect on cancer cells of PD 325901 can be determined by a sensitive imaging biomarker, 3'-deoxy-3'-[18F]fluorothymidine-positron emission tomography ([18F]FLT-PET). PD 325901 potently inhibited the proliferation of thyroid cancer cells with an IC50 of 0.06-0.78 µM. It also has synergistic inhibitory effects when combined with phosphatidylinositol 3-kinase (PI3K) or NF-κB pathway inhibitors in most thyroid cancer cell lines.

Blockade of MEK/ERK signaling by PD 325901 greatly enhances the cytotoxicity induced by arsenic trioxide (ATO) through a caspase-dependent mechanism in human myeloma cell lines and in tumor cells from patients with multiple myeloma.

Appearance

Supplied as an off-white solid

Purity

~95% (TLC, HPLC)

Melting Point

~116-118ºC

Solubility

Soluble in DMSO at 12mg/ml; soluble in ethanol at 6.3mg/ml with slight warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.

Elemental Analysis

Calculated C - 41.57% H - 3.43% F - 11.36% I - 25.3% N - 5.58%

Storage and Stability

Powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with DMSO or ethanol. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.

Purity

~95% (TLC, HPLC)

Form

Supplied as an off-white solid

Important Note

This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.

Product	Size	List	Your Price	Qty	Ext Price
Subtotal:	Subtotal:
Subtotal:	Subtotal:
Total Coupon Savings:	Total Coupon Savings:	()
Your cart is currently empty.
- Coupon Code

Product

Size

List

Your Price

Qty

Ext Price

Subtotal:

Total Coupon Savings:

()

Your cart is currently empty.

- Coupon Code

P3120-58 PD-325901, Free Base (PD 0325901, MEK1/2 Inhibitor III) CAS: 391210-10-9

CAS Number

Grade

Molecular Formula

Molecular Weight

EU Commodity Code

UN DOT Shipping

Shipping Temp

Storage Temp

N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2[(2-fluoro-4-iodophenyl)amino]-benzamide; PD 0325901, MEK1/2 Inhibitor III

References

USBio References

Pricing

Order

Cart Summary

Recently Viewed

Special Offers

Contact Us

Site Map

Technical Resources

Distributors

Payment Methods