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pd_meltingpoint:112-114 °C
Appearance:white powder
Purity:99%
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Biochem/physiol Actions |
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice. |
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Definition |
ChEBI: A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer). |
InChI:InChI=1/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
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The present disclosure relates to a) cry...
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![N-{[(R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy}-3,4-difluoro-2-[(2-fluoro-4-iodo-phenyl)amino]benzamide](/upload/2025/4/ec15577b-3604-4758-80f0-afe84f1d0461.png)
N-{[(R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy}-3,4-difluoro-2-[(2-fluoro-4-iodo-phenyl)amino]benzamide
PD0325901
| Conditions | Yield |
|---|---|
|
With
toluene-4-sulfonic acid;
In
methanol; water;
at 20 ℃;
for 18h;
|
70% |
|
With
hydrogenchloride; water;
In
toluene; acetonitrile;
at 20 - 25 ℃;
for 12 - 18h;
Product distribution / selectivity;
|
|
|
With
hydrogenchloride; water;
In
toluene;
for 2h;
pH=< 1;
Product distribution / selectivity;
|
|
|
With
hydrogenchloride;
In
water;
at 22 - 25 ℃;
|
|
|
With
hydrogenchloride;
In
water; toluene; acetonitrile;
at 5 ℃;
for 16h;
Large scale;
|
3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzoic acid
![(4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine](/upload/2025/4/0305e0dd-3f8d-4a88-8be3-f85b88de377f.png)
(4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine
PD0325901
| Conditions | Yield |
|---|---|
|
3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzoic acid; (4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine;
With
1,1'-carbonyldiimidazole;
In
ethanol; water; toluene; acetonitrile;
at 17 - 27 ℃;
for 7.5h;
With
hydrogenchloride;
In
water; toluene; acetonitrile;
for 20.0833h;
In
ethanol; water; toluene;
at 0 - 45 ℃;
|
|
|
3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzoic acid;
With
1,1'-carbonyldiimidazole;
In
acetonitrile;
at 22 ℃;
for 1.5h;
(4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine;
In
toluene; acetonitrile;
at 22 ℃;
for 6h;
|
|
|
3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzoic acid;
With
1,1'-carbonyldiimidazole;
In
acetonitrile;
at 220 ℃;
for 1.5h;
(4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine;
In
toluene; acetonitrile;
at 22 ℃;
for 6h;
With
hydrogenchloride;
In
water; toluene; acetonitrile;
|
3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzoic acid
(4R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethoxyamine
N-{[(R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy}-3,4-difluoro-2-[(2-fluoro-4-iodo-phenyl)amino]benzamide
(S)-O-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)hydroxylamine
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