Research Area
Product Type
United States ( Change Country )
CI-1040 (PD184352) Chemical Structure
AZD6244 (Selumetinib)
AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.
PD0325901
PD0325901 is MEK inhibitor and non-competitive with ATP, Kiapp of 1 nM against activated MEK1 and MEK2.
RDEA119 (BAY 869766)
MEK inhibitor with EC50 of 73 nM.
U0126-EtOH
U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
PD98059
PD 98059 is an inhibitor of MEK1 and MEK2 with IC50 values of 4 μM and 50 μM respectively.
AS703026
AS703026 is a highly selective and potent noncompetitive inhibitor of MEK1/2 with an IC50 range of 5-11 nM.
BIX 02188
BIX02188 is a MEK5-selective inhibitor with an IC50 of 0.8 ± 1.0 μM.
BIX 02189
BIX 02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
PD318088
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
AZD8330
AZD8330 is an orally active, selective MEK inhibitor with an IC50 of 7 nM.
Biological Activity
CI-1040 (PD184352) is a non-competitive inhibitor of MEK1/2 with a Ki of 300nM in vitro[1] CI-1040 inhibited MEK (as measured by phosphorylated ERK (p-ERK) levels) with a half-maximal inhibitory concentration (IC50) of 100–500nM in all cell lines tested. [2]
References on CI-1040 (PD184352)
- [1] NATURE MEDICINE JULY 1999;5：810－816
- [2] Nature 19 January 2006;439：358-362
Product Information
| Molecular Weight (WM): | 478.67 |
|---|---|
| Formula: | C17H14ClF2IN2O2 |
| CAS No.: | 212631-79-3 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥96mg/mL |
| Water <1mg/mL | |
| Ethanol ≥16mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
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Selleck's high quality products have been used in several published research findings, including the following:
BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation
The Antiproliferative Action of Progesterone in Uterine Epithelium Is Mediated by Hand2
A Feedback Loop between Androgen Receptor and ERK Signaling in Estrogen Receptor–Negative Breast Cancer.
Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer
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The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352. - The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352.
Data from [SCIENCE 2011 February;331:912-916] CI-1040 (PD184352) purchased from Selleck
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Click to enlarge
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CI-1040 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CI-1040 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
Data independently produced by Dr Zhang of Tianjin Medical University CI-1040 (PD184352) purchased from Selleck
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Click to enlarge
The effect of CI-1040 on cell viability of molecular apocrine lines. MTT assay to measure cell viability in MDAMB-453 cell line after treatment with CI-1040 (CI) at 2 to 25 μM concentrations. MTT assay to measure cell viability in HCC-1954 cell line after treatment with CI-1040 at 2 to 25 μM concentrations.
The effect of CI-1040 on cell viability of molecular apocrine lines. MTT assay to measure cell viability in MDAMB-453 cell line after treatment with CI-1040 (CI) at 2 to 25 μM concentrations. MTT assay to measure cell viability in HCC-1954 cell line after treatment with CI-1040 at 2 to 25 μM concentrations.
Data from [Breast Cancer Research 2011.April;13:R36] CI-1040 (PD184352) purchased from Selleck
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Click to enlarge
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CI-1040 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CI-1040 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
Data independently produced by Dr Zhang of Tianjin Medical University CI-1040 (PD184352) purchased from Selleck
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Click to enlarge
The bar chart represents the relative numbers of third-round colonies of primary hematopoietic cells transduced with MLL-AF9 with treatment of compound PD184352 (CI-1040, 10 UM, a MEK inhibitor) and SB216763 (10uM, GSK-3 inhibitor). The synergic effect between compounds CI-1040 and SB-216763 has been observed.
The bar chart represents the relative numbers of third-round colonies of primary hematopoietic cells transduced with MLL-AF9 with treatment of compound PD184352 (CI-1040, 10 UM, a MEK inhibitor) and SB216763 (10uM, GSK-3 inhibitor). The synergic effect between compounds CI-1040 and SB-216763 has been observed.
Data independently produced by Dr Shuo Dong of Baylor College of Medicine CI-1040 (PD184352) purchased from Selleck
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Western blot analysis to measure the phosphorylated and total ERK levels in MDA-MB-453 and HCC-1954 cell lines after treatment with CI-1040 (CI) at 10-μM concentration.
Western blot analysis to measure the phosphorylated and total ERK levels in MDA-MB-453 and HCC-1954 cell lines after treatment with CI-1040 (CI) at 10-μM concentration.
Data from [Neoplasia 2011.February;13:154–166] CI-1040 (PD184352) purchased from Selleck
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Relative expression of AR using RT-PCR in MDA-MB-453 and HCC-1954 cell lines after treatment with CI-1040 (MEK Inh) at 10-μMconcentration for 24 hours. Expression is relative to that of vehicle-treated cells (CTL). *P < .01 is for CI-1040 versus control. Error bars,±2 SEMs.
Relative expression of AR using RT-PCR in MDA-MB-453 and HCC-1954 cell lines after treatment with CI-1040 (MEK Inh) at 10-μMconcentration for 24 hours. Expression is relative to that of vehicle-treated cells (CTL). *P < .01 is for CI-1040 versus control. Error bars,±2 SEMs.
Data from [Neoplasia 2011.February;13:154–166] CI-1040 (PD184352) purchased from Selleck
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Synergistic effect of AR and mitogen-activated protein kinase kinase inhibitors on cell viability. (A) MTT assay to measure cell viability in MDA-MB-453 cell line after monotherapies and combination treatments with flutamide (FLU) and CI-1040 (CI) at 5 and 10 Μm concentrations. CTL: control. Error bars: ± 2 SEM. (B) Combination indices (CI) for flutamide and CI-1040 combination therapy in MDA-MB-453 cell line using MTT assay. Cell viability was measured after combination therapies with flutamide at 5 and 10 μM with each concentration of CI-1040 at 5 and 10 μM. The concentrations of FLU and CI-1040 monotherapies with an effect similar to that of each combination therapy are depicted. Error bars: ± 2 SEM. (C) Combination indices for flutamide and CI-1040 combination therapy in HCC-1954 cell line using MTT assay. Cell viability was measured after combination therapies with flutamide at 20 and 40 μM with each concentration of CI-1040 at 5 and 10 μM. (D) Combination indices for flutamide and CI-1040 combination therapy in HCC-202 cell line using MTT assay at concentrations described in Figure 2C.
Synergistic effect of AR and mitogen-activated protein kinase kinase inhibitors on cell viability. (A) MTT assay to measure cell viability in MDA-MB-453 cell line after monotherapies and combination treatments with flutamide (FLU) and CI-1040 (CI) at 5 and 10 Μm concentrations. CTL: control. Error bars: ± 2 SEM. (B) Combination indices (CI) for flutamide and CI-1040 combination therapy in MDA-MB-453 cell line using MTT assay. Cell viability was measured after combination therapies with flutamide at 5 and 10 μM with each concentration of CI-1040 at 5 and 10 μM. The concentrations of FLU and CI-1040 monotherapies with an effect similar to that of each combination therapy are depicted. Error bars: ± 2 SEM. (C) Combination indices for flutamide and CI-1040 combination therapy in HCC-1954 cell line using MTT assay. Cell viability was measured after combination therapies with flutamide at 20 and 40 μM with each concentration of CI-1040 at 5 and 10 μM. (D) Combination indices for flutamide and CI-1040 combination therapy in HCC-202 cell line using MTT assay at concentrations described in Figure 2C.
Data from [Neoplasia 2011.April;13:154–166] CI-1040 (PD184352) purchased from Selleck
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Click to enlarge
Combination indices (CI) for flutamide (FLU) and CI-1040 combination therapy in MDA-MB-453-R line using MTT assay. Therapies were carried out with flutamide at 5 and 10 μM with each concentration of CI-1040 at 5 and 10 μM (CI-5 and CL-10). The concentrations of fluatmide and CI-1040 monotherapies with an effect similar to that of each combination therapy are depicted. Error bars: ± 2SEM. Western blot analysis was used to measure the phosphorylated and total ERK levels in MDA-MB-453-R line following combination therapies with CI-1040 (5 μM)/flutamide (5 μM) and CI-1040 (5 μM)/flutamide (10 μM). RR values were measured relative to the untreated MDA-MB-453-R line. - Combination indices (CI) for flutamide (FLU) and CI-1040 combination therapy in MDA-MB-453-R line using MTT assay. Therapies were carried out with flutamide at 5 and 10 μM with each concentration of CI-1040 at 5 and 10 μM (CI-5 and CL-10). The concentrations of fluatmide and CI-1040 monotherapies with an effect similar to that of each combination therapy are depicted. Error bars: ± 2SEM. Western blot analysis was used to measure the phosphorylated and total ERK levels in MDA-MB-453-R line following combination therapies with CI-1040 (5 μM)/flutamide (5 μM) and CI-1040 (5 μM)/flutamide (10 μM). RR values were measured relative to the untreated MDA-MB-453-R line.
Data from [Breast Cancer Research 2011.April;13:R36] CI-1040 (PD184352) purchased from Selleck
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| The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352. |
Data from [SCIENCE 2011 February;331:912-916]
After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of CI-1040 for 3h,followed by 15-minute stimolation of 100ng/ml EGF
|
Data independently produced by Dr Zhang of Tianjin Medical University
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