Equivalent to the IC50 for wild-type PI3K¦Á, PKI-402 inhibits E545K and H1047R PI3K¦Á mutants with IC50 of 3 nM. In a panel of 236 human protein kinases, PKI-402 only displays inhibitory activity against C-Raf and B-Raf with IC50 of 7 ¦ÌM, and displays little activity against all other kinases with IC50 of > 10 ¦ÌM. PKI-402 inhibits the growth of human tumor cell lines with IC50 of 6-349 nM. Consistently, PKI-402 inhibits phosphorylation of PI3K and mTOR effector proteins, particularly phosphorylated Akt (p-Akt) at T308 and S473 with IC50 of <10 nM and <30 nM, respectively. PKI-402 inhibits both p70S6K and 4EBP1 phosphorylation with IC50 of <10 nM. PKI-402 inhibits Akt phosphorylation of PRAS40 at T246 with IC50 of <30 nM, and inhibits Akt phosphorylation of ENOS at S1177 and GSK3¦Á/GSK3¦Â at S9/S21 with IC50 of <10 nM. In MDAMB-361, a breast tumor line with mutant PI3K-¦Á (E545K) and elevated levels of Her2 receptor, PKI-402 treatment induces cleaved poly(ADP-ribose) polymerase (PARP), a marker for apoptosis. Less than 10% of MDAMB-361 cells exposed to PKI-402 at 0.3 ¦ÌM (or higher) for 24 hours remain viable.

 June 21, 2017

prudect name : Equivalent to the IC50 for wild-type PI3K¦Á, PKI-402 inhibits E545K and H1047R PI3K¦Á mutants with IC50 of 3 nM. In a panel of 236 human protein kinases,…

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prudect name : Prostaglandin E2Synonyms: DinoprostoneCAS NO: 363-24-6Molecular Formula: C20H32O5Molecular Weight: 352.47Purity: 99%Solubility: Storage: −20°C

prudect name : Prostaglandin E2 Synonyms: DinoprostoneCAS NO: 363-24-6Molecular Formula: C20H32O5Molecular Weight: 352.47Purity: 99%Solubility: Storage: −20°C 2 years web site: www.medchemexpress.com

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prudect name : PerampanelSynonyms: CAS NO: 380917-97-5Molecular Formula: C23H15N3OMolecular Weight: 349.38Purity: 98% minSolubility: in DMSOStorage:

prudect name : Perampanel Synonyms: CAS NO: 380917-97-5Molecular Formula: C23H15N3OMolecular Weight: 349.38Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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prudect name : PregnenoloneSynonyms: CAS NO: 145-13-1Molecular Formula: C21H32O2Molecular Weight: 316.48Purity: 99% minSolubility: Storage: −20°C

prudect name : Pregnenolone Synonyms: CAS NO: 145-13-1Molecular Formula: C21H32O2Molecular Weight: 316.48Purity: 99% minSolubility: Storage: −20°C web site: www.medchemexpress.com

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prudect name : ProgesteroneSynonyms: CAS NO: 57-83-0Molecular Formula: C21H30O2Molecular Weight: 314.47Purity: 98% minSolubility: Storage: −20°C

prudect name : Progesterone Synonyms: CAS NO: 57-83-0Molecular Formula: C21H30O2Molecular Weight: 314.47Purity: 98% minSolubility: Storage: −20°C web site: www.medchemexpress.com

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VEGFR enzyme assays for VEGGR1,VEGFR2, and VEGFR3 were running in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Pazopanib showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFR beta, c-Kit, FGF-R1, and c-fms with IC50¡¯s of 84, 74, 140,and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib potently inhibited VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM. The cytochrome P450 profile was also improved with inhibition >10 ¦ÌM against the isozymes tested, with the exception of 2C9 (7.9 ¦ÌM).

prudect name : VEGFR enzyme assays for VEGGR1,VEGFR2, and VEGFR3 were running in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein…

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Plerixafor inhibits CXCL12-mediated chemotaxis with a potency slightly better than its affinity for CXCR4.Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, Nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF¨CCEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7

prudect name : Plerixafor inhibits CXCL12-mediated chemotaxis with a potency slightly better than its affinity for CXCR4.Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits…

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PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.PD173074 is a cell-permeable pyridopyrimidine compound. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. PD173074 inhibits PDGFR and c-Src only at much higher concentration (IC50 = 17.6 µM, 19.8 µM, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 µM. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50 <5 nM) and overexpressed VEGFR2 (IC50 <200 nM) in NIH3T3 cells in vitro, and FGF- and VEGF-induced angiogenesis in mice in vivo.

prudect name : PD173074 is a potent ATP-competitive, reversible FGFR and VEGFR inhibitor with IC50 of 5, 21.5 and ~100 nM for FGFR3, FGFR1 and VEGFR2, respectively.PD173074 is a cell-permeable…

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5-[3-[3-(2-Chloro-4-fluorophenoxy)-1-azetidinyl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxypyridine

prudect name : 5-[3-[3-(2-Chloro-4-fluorophenoxy)-1-azetidinyl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxypyridinePF 3274167 Synonyms: CAS NO: 900510-03-4Molecular Formula: C19H19ClFN5O3Molecular Weight: 419.84Purity: 98% minSolubility: In DMSOStorage: −20°C 2 years web site: www.medchemexpress.com

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PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 ¦ÌM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells.

prudect name : PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435…

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