NSC 852426
NSC 852426 is a PDGFRα/VEGFR-2 inhibitor with IC50 values of 1.179 μM and 1.818 μM, respectively. NSC 852426 inhibits AKT and ERK1/2 phosphorylation, upregulates P53, BAX, and caspase-3 while inhibiting Bcl-2, and induces intrinsic mitochondrial apoptosis. NSC 852426 exhibits selective antiproliferative and cytotoxic effects against multiple cancer cell lines, and shows moderate selectivity for leukemia and colon cancer subgroups. NSC 852426 can be used in cancer-related research, such as leukemia and colon cancer.
For research use only. We do not sell to patients.
- Formula: C22H17N3O4
- Molecular Weight:387.39
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
VEGFR2 1.818 μM (IC50) |
PDGFRα 1.179 μM (IC50) |
Caspase 3 |
Bax |
Bcl-2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | GI50 |
2.33 μM
|
Antiproliferative activity against human CCRF-CEM cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human CCRF-CEM cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HL-60(TB) | GI50 |
3.67 μM
|
Antiproliferative activity against human HL-60(TB) cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HL-60(TB) cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| K562 | GI50 |
3.13 μM
|
Antiproliferative activity against human K-562 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human K-562 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| MOLT-4 | GI50 |
2.07 μM
|
Antiproliferative activity against human MOLT-4 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MOLT-4 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| RPMI-8226 | GI50 |
0.69 μM
|
Antiproliferative activity against human RPMI-8226 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human RPMI-8226 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SR | GI50 |
0.28 μM
|
Antiproliferative activity against human SR cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SR cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| A549 | GI50 |
10.4 μM
|
Antiproliferative activity against human A549/ATCC cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human A549/ATCC cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| EKVX | GI50 |
10.6 μM
|
Antiproliferative activity against human EKVX cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human EKVX cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HOP-62 | GI50 |
4.99 μM
|
Antiproliferative activity against human HOP-62 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HOP-62 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HOP-92 | GI50 |
3.35 μM
|
Antiproliferative activity against human HOP-92 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HOP-92 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| NCI-H226 | GI50 |
6.62 μM
|
Antiproliferative activity against human NCI-H226 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human NCI-H226 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| NCI-H23 | GI50 |
3.71 μM
|
Antiproliferative activity against human NCI-H23 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human NCI-H23 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| NCI-H322M | GI50 |
20.1 μM
|
Antiproliferative activity against human NCI-H322M cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human NCI-H322M cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| NCI-H460 | GI50 |
6.81 μM
|
Antiproliferative activity against human NCI-H460 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human NCI-H460 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| NCI-H522 | GI50 |
1.04 μM
|
Antiproliferative activity against human NCI-H522 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human NCI-H522 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| COLO 205 | GI50 |
18.7 μM
|
Antiproliferative activity against human COLO205 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human COLO205 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HCC 2998 | GI50 |
2.04 μM
|
Antiproliferative activity against human HCC-2998 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HCC-2998 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HCT-116 | GI50 |
1.66 μM
|
Antiproliferative activity against human HCT-116 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HCT-116 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HCT-15 | GI50 |
3.74 μM
|
Antiproliferative activity against human HCT-15 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HCT-15 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| HT-29 | GI50 |
4.75 μM
|
Antiproliferative activity against human HT29 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HT29 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| KM12 | GI50 |
2.37 μM
|
Antiproliferative activity against human KM12 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human KM12 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SW-620 | GI50 |
4.31 μM
|
Antiproliferative activity against human SW-620 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SW-620 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SF-268 | GI50 |
5.69 μM
|
Antiproliferative activity against human SF-268 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SF-268 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SF-295 | GI50 |
7.49 μM
|
Antiproliferative activity against human SF-295 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SF-295 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SF-539 | GI50 |
2.11 μM
|
Antiproliferative activity against human SF-539 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SF-539 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SNB-19 | GI50 |
12.0 μM
|
Antiproliferative activity against human SNB-19 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SNB-19 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SNB-75 | GI50 |
13.8 μM
|
Antiproliferative activity against human SNB-75 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SNB-75 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| U-251 | GI50 |
2.46 μM
|
Antiproliferative activity against human U251 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human U251 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| LOX IMVI | GI50 |
2.97 μM
|
Antiproliferative activity against human LOX IMVI cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human LOX IMVI cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| Malme-3M | GI50 |
17.3 μM
|
Antiproliferative activity against human MALME-3M cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MALME-3M cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| M14 | GI50 |
3.96 μM
|
Antiproliferative activity against human M14 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human M14 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| MDA-MB-435 | GI50 |
5.17 μM
|
Antiproliferative activity against human MDA-MB-435 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MDA-MB-435 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SK-MEL-2 | GI50 |
6.98 μM
|
Antiproliferative activity against human SK-MEL-2 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SK-MEL-2 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SK-MEL-28 | GI50 |
13.9 μM
|
Antiproliferative activity against human SK-MEL-28 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SK-MEL-28 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SK-MEL-5 | GI50 |
10.6 μM
|
Antiproliferative activity against human SK-MEL-5 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SK-MEL-5 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| UACC-257 | GI50 |
4.54 μM
|
Antiproliferative activity against human UACC-257 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human UACC-257 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| UACC-62 | GI50 |
7.70 μM
|
Antiproliferative activity against human UACC-62 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human UACC-62 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| IGROV-1 | GI50 |
6.20 μM
|
Antiproliferative activity against human IGROV1 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human IGROV1 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| OVCAR-3 | GI50 |
7.07 μM
|
Antiproliferative activity against human OVCAR-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human OVCAR-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| OVCAR-4 | GI50 |
8.57 μM
|
Antiproliferative activity against human OVCAR-4 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human OVCAR-4 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| OVCAR-5 | GI50 |
24.6 μM
|
Antiproliferative activity against human OVCAR-5 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human OVCAR-5 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| OVCAR-8 | GI50 |
5.90 μM
|
Antiproliferative activity against human OVCAR-8 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human OVCAR-8 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SK-OV-3 | GI50 |
2.41 μM
|
Antiproliferative activity against human SK-OV-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SK-OV-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| 786-0 | GI50 |
3.77 μM
|
Antiproliferative activity against human 786-0 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human 786-0 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| A498 | GI50 |
2.13 μM
|
Antiproliferative activity against human A498 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human A498 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| CAKI-1 | GI50 |
8.17 μM
|
Antiproliferative activity against human CAKI-1 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human CAKI-1 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| RXF 393 | GI50 |
2.46 μM
|
Antiproliferative activity against human RXF 393 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human RXF 393 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| SN12C | GI50 |
5.97 μM
|
Antiproliferative activity against human SN12C cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human SN12C cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| TK-10 | GI50 |
9.55 μM
|
Antiproliferative activity against human TK-10 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human TK-10 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| UO-31 | GI50 |
10.9 μM
|
Antiproliferative activity against human UO-31 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human UO-31 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| PC-3 | GI50 |
8.93 μM
|
Antiproliferative activity against human PC-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human PC-3 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| DU-145 | GI50 |
6.45 μM
|
Antiproliferative activity against human DU-145 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human DU-145 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| MCF7 | GI50 |
2.13 μM
|
Antiproliferative activity against human MCF7 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MCF7 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| MDA-MB-231 | GI50 |
13.8 μM
|
Antiproliferative activity against human MDA-MB-231/ATCC cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MDA-MB-231/ATCC cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| Hs-578T | GI50 |
2.59 μM
|
Antiproliferative activity against human HS 578T cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human HS 578T cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| BT-549 | GI50 |
2.23 μM
|
Antiproliferative activity against human BT-549 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human BT-549 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| T47D | GI50 |
3.47 μM
|
Antiproliferative activity against human T-47D cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human T-47D cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| MDA-MB-468 | GI50 |
2.33 μM
|
Antiproliferative activity against human MDA-MB-468 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
Antiproliferative activity against human MDA-MB-468 cells assessed as 50% growth inhibition after 48 hrs by NCI five-dose assay.
|
42748748 |
| WI-38 | IC50 |
146.64 μM
|
Cytotoxicity against normal human lung fibroblast WI-38 cells assessed as 50% inhibitory concentration by MTT assay.
Cytotoxicity against normal human lung fibroblast WI-38 cells assessed as 50% inhibitory concentration by MTT assay.
|
42748748 |
| Vero | IC50 |
209.16 μM
|
Cytotoxicity against african green monkey kidney epithelial VERO cells assessed as 50% inhibitory concentration by MTT assay.
Cytotoxicity against african green monkey kidney epithelial VERO cells assessed as 50% inhibitory concentration by MTT assay.
|
42748748 |
In Vitro
NSC 852426 (0.01-100 mM; 48 h) had a full-panel MG-MID GI50 of 6.18 μM, with moderate selectivity for leukemia (SI 3.04) and colon cancer (SI 4.57), and GI50 values of 0.28 μM in leukemia SR and 1.66 μM in colon HCT-116[1].
NSC 852426 showed low cytotoxicity in normal WI-38 (IC50 146.64 μM) and VERO (IC50 209.16 μM) cells, with a wide safety window[1].
NSC 852426 inhibited p-AKT to 0.286-fold of the control and p-ERK1/2 to 0.291-fold of the control in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:NCI 60 human tumor cell lines (leukemia, NSCLC, colon, CNS, melanoma, ovarian, renal, prostate, breast)
-
Concentration:11 μM
-
Incubation Time:48 h
-
Result:Exhibited NCI‑60 one‑dose growth‑inhibition (GI%) profiles covering diverse human tumour sub‑panels.
Exhibited pronounced growth‑inhibitory potency against the majority of leukemia cell lines, including CCRF‑CEM, HL‑60(TB), MOLT‑4, RPMI‑8226 and SR.
Exhibited strong cytotoxic responses for partial colon, melanoma and ovarian cancer cell strains such as HCT‑116, LOX IMVI and SK‑OV‑3.
Exhibited heterogeneous antiproliferative outcomes across NSCLC, CNS, renal, prostate and breast cancer cell models, with cell‑line‑dependent high or low growth‑inhibition magnitudes.
-
Cell Line:NCI 60 human tumor cell lines (nine tumor subpanels)
-
Concentration:0.01, 0.1, 1, 11, 100 mM
-
Incubation Time:48 h
-
Result:Displayed NCI‑60 five‑dose antiproliferative GI50 (micromolar) data across nine human tumour sub‑panels.
Displayed outstanding potency against leukemia cell lines, with sub‑micromolar GI50 values for RPMI‑8226 and SR, and leukemia sub‑panel MG‑MID value of 2.03 micromolar.
Displayed favourable overall activity against colon, breast and renal cancer sub‑panels, whose respective MG‑MID values reached 5.37, 4.43 and 5.37 micromolar.
Displayed relatively weaker average inhibitory potency for NSCLC, CNS, melanoma, ovarian and prostate cancer sub‑panels, with corresponding MG‑MID values ranging from 7.21 to 8.12 micromolar.
Displayed full‑panel MG‑MID GI50 of 6.18 micromolar, and yielded selectivity indices of 3.04 for leukemia and 4.57 for colon cancer, while presenting low‑to‑moderate selectivity indices for other tumour sub‑panels.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
-
Molecular Weight 387.39
-
Formula C22H17N3O4
-
SMILES
O=C(NC1=CC=CC=C1)NC2=CC=C(C(/C=C/C3=CC=C([N+]([O-])=O)C=C3)=O)C=C2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)