PF-05212384
- CAS No.
- 1197160-78-3
- Chemical Name:
- PF-05212384
- Synonyms
- CS-46;PKI587;PF-05212384;GEDATOLISIB;PKI-587;PKI 587 PF 05212384;PF-05212384 (PKI-587);PF-05212384 USP/EP/BP;PKI-587 ( Gedatolisib );GEDATOLISIB;PF-05212384;Gedatolisib (PF-05212384, PKI-587)
- CBNumber:
- CB32500950
- Molecular Formula:
- C32H41N9O4
- Molecular Weight:
- 615.73
- MDL Number:
- MFCD16875679
- MOL File:
- 1197160-78-3.mol
- MSDS File:
- SDS
| Melting point | 226-227°C |
|---|---|
| Density | 1.364 |
| storage temp. | Refrigerator |
| solubility | DMSO |
| pka | 13.97±0.70(Predicted) |
| form | Solid |
| color | Off-White |
| FDA UNII | 96265TNH2R |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| HS Code | 29349990 |
PF-05212384 price More Price(25)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 14567 | PF-05212384 ≥98% | 1197160-78-3 | 1mg | $37 | 2024-03-01 | Buy |
| Cayman Chemical | 14567 | PF-05212384 ≥98% | 1197160-78-3 | 5mg | $161 | 2024-03-01 | Buy |
| Cayman Chemical | 14567 | PF-05212384 ≥98% | 1197160-78-3 | 10mg | $283 | 2024-03-01 | Buy |
| Tocris | 4823 | PF05212384 ≥98%(HPLC) | 1197160-78-3 | 10 | $275 | 2021-12-16 | Buy |
| TRC | D461135 | N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N''-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-urea | 1197160-78-3 | 50mg | $670 | 2021-12-16 | Buy |
PF-05212384 Chemical Properties,Uses,Production
Description
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
Chemical Properties
Off-White Solid
Uses
This compound shows inhibitory activity against PI3K-α, PI3K-γ and mTOR. Potent PI3K/mTOR Dual Inhibitor.
Biological Activity
pf-05212384 is an inhibitor of pi3k/mtor with ic50 values of 0.4nm, 6nm, 8nm, 6nm and 1.4nm for pi3kα, pi3kβ, pi3kγ, pi3kδ and mtor, respectively [1].pf-05212384 is a pan-pi3k/mtorinhibitor and shows to be highly selective for pi3k and mtor. besides the wt p13k, pf-05212384 can also inhibit mutant p13k with ic50 values of 0.6nm for both h1047r and e545k mutants. in cellular assay, pf-05212384 potently inhibits tumor growth in mda-361 and pc3-mm2 cell lines with ic50 values of 4nm and 13.1nm, respectively. meanwhile, pf-05212384 suppresses the phosphorylation of pi3k/mtor signaling pathway proteins in cells. it inhibits the phosphorylation of akt as well as the akt effector proteins including gsk3 kinase, enos and pras 40. moreover, pf-05212384 has potent anti-tumor activity in a variety of xenograft models including h1975, bt474, hct116, h1975 and u87mg [1, 2]
Enzyme inhibitor
This dual PI3K/mTOR (phosphoinositide-3-kinase and mammalian target of rapamycin) signal-transduction pathway inhibitor and antineoplastic agent (F.Wt. = 615.73; CAS 1197160-78-3); Solubility (25°C): 2 mg/mL DMSO, <1 mg/mL Water), also known as PF-05212384 and systematically as 1-(4- (4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino- 1,3,5-triazin-2-yl)phenyl)urea, inhibits PI3K-α, PI3K-γ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 also inhibits mutant forms of PI3Kα, including the PI3Kα-H1047R and PI3Kα-E545K with IC50 of 0.6 nM and 0.6 nM, respectively.
References
[1] venkatesan a m, dehnhardt c m, delos santos e, et al. bis (morpholino-1, 3, 5-triazine) derivatives: potent adenosine 5′-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (pki-587), a highly efficacious dual inhibitor. journal of medicinal chemistry, 2010, 53(6): 2636-2645.
[2] mallon r, feldberg l r, lucas j, et al. antitumor efficacy of pki-587, a highly potent dual pi3k/mtor kinase inhibitor. clinical cancer research, 2011, 17(10): 3193-3203.
PF-05212384 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | sales@capotchem.com | China | 29797 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22968 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63711 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 47465 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
View Lastest Price from PF-05212384 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2021-10-08 | Gedatolisib;PKI-587
1197160-78-3
|
US $200.00-0.00 / g | 1g | 98%+ | 100kgs | Wuhan Nutra Biotechnology Co.,Ltd | |
 |
2019-07-06 | PF-05212384
1197160-78-3
|
US $2.00 / kg | 1kg | 99% | 100kg | Career Henan Chemical Co |
-
- Gedatolisib;PKI-587
1197160-78-3
- US $200.00-0.00 / g
- 98%+
- Wuhan Nutra Biotechnology Co.,Ltd
-
- PF-05212384
1197160-78-3
- US $2.00 / kg
- 99%
- Career Henan Chemical Co