Crenolanib | PDGFR and FLT3 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $195.00 |
Crenolanib (670220-88-9) is a potent inhibitor of PDGFR (Kd for α = 2.1 nM; β = 3.2 nM) and FLT3 (Kd = 0.74 nM).1 Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432 as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+ AML murine xenograft model.4
References/Citations:
1) Lewis et al. (2009) Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers; J. Clin. Oncol. 27 5262
2) Smith et al. (2014) Crenolanib is a selective type I pan-FLT3 inhibitor; Proc. Natl. Acad. Sci. USA 111 5319
3) Heinrich et al. (2012) Crenolanib Inhibits Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors; Clin. Cancer Res. 18 4375
4) Jetani et al. (2018) CAR T-cells targeting FLT3 have potent activity against FLT-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib; Leukemia 32 1168
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
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Crenolanib (670220-88-9) is a potent inhibitor of PDGFR (Kd for α = 2.1 nM; β = 3.2 nM) and FLT3 (Kd = 0.74 nM).1 Crenolanib is a type I inhibitor binding only to the active kinase conformation. It showed potent activity against imatinib-resistant PDGFRα mutations D842I, D842V, D842Y, DI842-843M, and deletion I8432 as well as FLT3/ITD and FLT3/D835 mutants3. Crenolanib acted synergistically with FLT3-CAR T-cells in a FLT3-ITD+ AML murine xenograft model.4
References/Citations:
1) Lewis et al. (2009) Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers; J. Clin. Oncol. 27 5262
2) Smith et al. (2014) Crenolanib is a selective type I pan-FLT3 inhibitor; Proc. Natl. Acad. Sci. USA 111 5319
3) Heinrich et al. (2012) Crenolanib Inhibits Drug-Resistant PDGFRA D842V Mutation Associated with Imatinib-Resistant Gastrointestinal Stromal Tumors; Clin. Cancer Res. 18 4375
4) Jetani et al. (2018) CAR T-cells targeting FLT3 have potent activity against FLT-ITD+ AML and act synergistically with the FLT3-inhibitor crenolanib; Leukemia 32 1168
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