PF-04691502
- CAS No.
- 1013101-36-4
- Chemical Name:
- PF-04691502
- Synonyms
- CS-305;CS-2640;PF4691502;PF-04691502;PF 04691502; PF04691502;PF-04691502 ISO 9001：2015 REACH;PF-04691502, 98%, a potent and selective inhibitor of PI3K and mTOR kinases;2-Amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3;2-amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one;2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
- CBNumber:
- CB22589602
- Molecular Formula:
- C22H27N5O4
- Molecular Weight:
- 425.48
- MOL File:
- 1013101-36-4.mol
- Modify Date:
- 2023/5/18 11:31:15
PF-04691502 price More Price(2)
PF-04691502 Chemical Properties,Uses,Production
Chemical Properties
Pale Yellow Solid
Uses
PF-04691502 is an ATP-competitive PI3K/mTOR inhibitor with IC50 of 32 nM and also inhibits Akt T308/S473 with IC50 of 7.5 nM/3.8 nM.
Enzyme inhibitor
This ATP-competitive PI3K/mTOR dual inhibitor (FW = 325.49 g/mol; CAS 1013101-36-4; Solubility = 14 mg/mL DMSO, < 1 mg/ML H2O), also systematically named 2-amino-8-((1R,4R)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)- one, potently inhibits recombinant Class-I PI3Kα (Ki = 1.8 nM), PI3Kβ (Ki = 2.1 nM), PI3Kδ (Ki = 1.6 nM), PI3Kγ (Ki = 1.9 nM), and mTOR (Ki = 16 nM) in biochemical assays, with little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK. PF-04691502 also suppresses avian fibroblast transformation mediated by wild-type PI3K γ, δ, or mutant PI3Kα. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF- 04691502 reduces phosphorylation of AKT T308 (IC50 = 7.5–47 nM) and AKT S473 (IC50 = 3.8–20 nM) and inhibits cell proliferation (IC50 = 180– 310 nM). PF-04691502 also inhibite mTORC1 activity within cells, asmeasured by PI3K-independent, nutrient-stimulated assay (IC50 = 32 nM) and inhibited the activation of PI3K and mTOR downstream effectors, including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. Shortterm exposure to PF-04691502 predominantly inhibits PI3K, whereas mTOR inhibition persists for 24 to 48 hours. PF-04691502 also induces cell cycle G1 arrest, concomitant with upregulation of p27 Kip1 and reduction of retinbalstoma protein, or Rb. At doses below the maximal tolerable dose, PD-0325901 potently inhibits tumor growth, when Kras and/or PI3K are drivers of tumor growth and progression.
PF-04691502 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29898 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | China | 23556 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 25196 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | China | 3136 | 58 | Inquiry |
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