| Cat. No. |
Product Name |
CAS No. |
Information |
| H8967 |
Seralutinib
|
1619931-27-9 |
Seralutinib is a potent small molecule PDGFR kinase inhibitor, being developed as an orally inhaled treatment for PAH to directly target the diseased pulmonary arterioles. |
| H8923 |
BLU-263
|
2505078-08-8 |
BLU-263 is a novel Protein tyrosine kinase inhibitors. |
| H7956 |
Toceranib
|
356068-94-5 |
An ATP-competitive inhibitor of RTKs, including VEGFR, FGFR, PDGFR, and Kit; inhibits phosphorylation of WT Kit in the presence of stem cell factor at concentrations as low as 0.01 uM; disrupts function of all forms of mutant Kit in cells. |
| H7955 |
Sunitinib
|
557795-19-4 |
A multi-targeted RTK inhibitor that targets VEGFR2 (Flk-1) and PDGFRβ with Ki of 8 nM and 9 nM respectively; displays >10-fold higher selectivity over FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and Src; also inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM; regresses FLT3-ITD tumors in the subcutaneous tumor xenograft model. |
| H7954 |
SU 16f
|
251356-45-3 |
SU 16f is a potent and selective PDGFRβ inhibitor with IC50 of 10 nM, displays >14-fold, >229-fold and >10,000-fold selectivity over VEGFR2, FGFR1 and EGFR respectively; inhibits proliferation of HUVEC and NIH3T3 cells in vitro (IC50 =0.11 uM). |
| H7953 |
N-Desethyl Sunitinib
|
356068-97-8 |
The active metabolite of sunitinib, which is an oral, small-molecule, multi-targeted RTKs inhibitor for the treatment of RCC and imatinib-resistant GIST. |
| H7952 |
MK-1
|
1026307-65-2 |
MK1 is a small molecule inducer of megakaryopoiesis (EC90=750 nM) that induces the differentiation of common myeloid progenitors (CMP) to megakaryocytes, does not adversely affect erythrocyte differentiation; a PDGFR inhibitor that inhibits PDGF-CC-mediated PDGFR phosphorylation in U138-malignant glioma cells, also inhibits the PDGF-CC-induced phosphorylation of PLCγ1, a major downstream target of PDGFR. |
| H7951 |
JNJ-10198409
|
627518-40-5 |
JNJ-10198409 is a highly potent, selective PDGFRβ inhibitor with IC50 of 4.2 nM; displays >10-fold selectivity over PDGFRα (IC50=45 nM), and 5-fold over c-ABL (IC50=22 nM), >500-fold over a panel of kinases; also has modest activity against have modest activity against c-Src/Lck/Fyn (IC50=185/100/378 nM); shows potent antiproliferative activity for human tumor cell lines (IC50=33 nM); regulates Oct4 and Nanog expression, cell shape, and mesenchymal stem cell potency. |
| H7950 |
CP-673451
|
343787-29-1 |
CP-673451 is a potent, selective, orally acitve PDGFR inhibitor with IC50 of 1 and 10 nM for PDGFR-α and PDGFR-β, respectively; inhibits PDGFR-β autophosphorylation with IC50 of 1 nM in cell-based assyas, displays >450-fold selectivity over other angiogenic receptors, including VEGFR-1, VEGFR-2, TIE-2, and FGFR-2; inhibits PDGFR phosphorylation in tumor xenografts and inhibits multiple types tumor growth in vivo; also robustly inhibits centrosome clusterin, induces mitotic spindle multipolarity by activation of the actin-severing protein cofilin in cancer cells. |
| H7949 |
CGP-53716
|
152459-94-4 |
A potent protein tyrosine kinase inhibitor that shows selectivity for PDGFR in vitro and in cells; shows selectivity for inhibition of PDGF-mediated events such as PPDGFR autophosphorylation, cellular tyrosine phosphorylation, and c-Fos mRNA induction in response to PDGF stimulation of intact cells. |
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