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Home > Inhibitors & Agonists > PI3K/Akt/mTOR > PI3K

PF-06843195

  Cat. No.:  DC44213   Featured
Chemical Structure
2067281-51-8
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More than 5000 active chemicals with high quality for research!
Field of application
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2067281-51-8
Chemical Name: Unii-75658jdg29
Synonyms: PF-06843195;75658JDG29;2,2-difluoroethyl (3S)-3-{[2'-amino-5-fluoro-2-(morpholin-4-yl)[4,5'-bipyrimidin]-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate;US9758538, Example 2;BDBM340314;(Scheme A): Preparation of 2,2-difluoroethyl (3S)-3-{[2'-amino-5-fluoro-2-(morpholin-4-yl)-4,5'-bipyrimidin-6-yl]amino}-3-(hydroxymethyl)pyrrolidine-1-carboxylate;1-Pyrrolidinecarboxylic acid, 3-((2'-amino-5-fluoro-2-(4-morpholinyl)(4,5'-bip;Unii-75658jdg29
SMILES: FC1=C(C2=C([H])N=C(N([H])[H])N=C2[H])N=C(N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])N=C1N([H])[C@]1(C([H])([H])O[H])C([H])([H])N(C(=O)OC([H])([H])C([H])(F)F)C([H])([H])C1([H])[H]
Formula: C20H25F3N8O4
M.Wt: 498.4589
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC71172 NVP-CLR457 NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
DC70705 PQR514 PQR514 is a potent selective pan-PI3K inhibitor with binding Ki of 2.2 and 33 nM for p110α and mTOR, repectively.PQR514 inhibits phosphorylated S6 ribosomal protein (pS6, Ser235/236) and phosphorylation PKB Ser473 in A2058 cells with IC50 of 17 and 68 nM, respectively.PQR514 displays negligible interference with protein kinase activities at 10 uM in a KINOMEScan panel.PQR514 exhibits growth inhibition in vitro across a panel of 66 tumor cells with GI50 of 0.25 uM.PQR514 demonstrates significant antitumor activity aginst OVCAR-3 human ovarian cancer xenograft model in BALB/c nude mice.
DC44213 PF-06843195 PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
DC7228 PF-04691502 PF-04691502 is an ATP-competitive PI3K(α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.
DC1068 XL147 analogue(PI3K inhibitor X) XL147 analogue (SAR245408) is a selective and reversible class I PI3K inhibitor for wild type and mutant p110α with IC50 of 40 nM and 40 nM, respectively.
DC10019 VPS34 inhibitor 1 (Compound 19, PIK-III analogue) VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
DC8884 Voxtalisib (XL765, SAR245409) Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.
DC5181 Voxtalisib Analogue Voxtalisib (SAR245409, XL765) Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.
DC9311 Serabelisib(TAK-117,INK1117,MLN1117) TAK-117(INK1117,MLN1117) is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity.
DC10140 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K and BRD4with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively.
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