CAS NO. |
Products Name |
670220-88-9 |
Crenolanib (CP-868596) |
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Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB2, and Src |
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154447-35-5 |
NU7026 |
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NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. |
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952021-60-2 |
PF-477736 |
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PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. Phase 1. |
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1489389-18-5 |
CCT245737 |
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CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM. target:CHK1; IC 50: 30-220nM; In vitro: CCT245737 shows <50% inhibition at 10 μM for 85/121 kinases, representing a selectivity for CHK1 inhibition of >5000-fold over these enzymes. [1] CCT245737 enhanced gemcitabine antitumor activity to a greater degree than for higher doses of either agent alone, without increasing toxicity. [2] In vivo: CCT2457374 shows an increase in plasma and tumoconcentrations between 3-100 mg/kg po. [1 |
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