PF-4989216
- Product Name
- PF-4989216
- CAS No.
- 1276553-09-3
- Chemical Name
- PF-4989216
- Synonyms
- CS-1547;PF-4989216;PF-4989216, 10 mM in DMSO;PF-4989216;PF 4989216;PF4989216;Apoptosis,inhibit,Phosphoinositide 3-kinase,PF4989216,PF-4989216,PI3K,Inhibitor;4-(4-Cyano-2-fluorophenyl)-2-morpholino-5-(1H-1,2,4-triazol-5-yl)thiophene-3-carbonitrile;4-(4-cyano-2-fluorophenyl)-2-morpholin-4-yl-5-(1H-1,2,4-triazol-5-yl)thiophene-3-carbonitrile;3-Thiophenecarbonitrile, 4-(4-cyano-2-fluorophenyl)-2-(4-morpholinyl)-5-(1H-1,2,4-triazol-5-yl)-
- CBNumber
- CB92667635
- Molecular Formula
- C18H13FN6OS
- Formula Weight
- 380.4
- MOL File
- 1276553-09-3.mol
PF-4989216 Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- crystalline solid
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 19308
- Product name
- PF-4989216
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 19308
- Product name
- PF-4989216
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $172
- Updated
- 2024/03/01
- Product number
- 19308
- Product name
- PF-4989216
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $299
- Updated
- 2024/03/01
- Product number
- 19308
- Product name
- PF-4989216
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $533
- Updated
- 2024/03/01
- Product number
- CS-5205
- Product name
- PF-4989216
- Purity
- 99.43%
- Packaging
- 50mg
- Price
- $696
- Updated
- 2021/12/16
PF-4989216 Chemical Properties,Usage,Production
Uses
PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
Biological Activity
the constitutive activation of phosphoinositide 3-kinase (pi3k) occurs frequently in many human tumors through either gene mutation in the p110a catalytic subunit of pi3k or functional loss of tumor suppressor pten. patients with small-cell lung cancer have very poor prognosis and survival rates such that an effective targeted therapy is in strong demand for these patients. pf-4989216 is a selective oral pi3k inhibitor.
in vitro
pf-4989216 inhibited pi3k downstream signaling and led to apoptosis induction, and inhibition in cell viability, transformation, and xenograft tumor growth in small-cell lung cancer (sclc) harboring pik3ca mutation. in sclc with pten loss, pf-4989216 also inhibited pi3k signaling but did not induce bcl2-interacting mediator-mediated apoptosis nor was there any effect on cell viability or transformation [1].
in vivo
the mouse in vivo results indicate a good correlation between in vitro and in vivo efficacy, and further confirm that pf-4989216 is an effective drug candidate capable of inducing antitumor activity in mice bearing human sclc tumors with pik3ca mutation [1].
target
| Target | Value |
| p110δ (Cell-free assay) | 1 nM |
| p110α (Cell-free assay) | 2 nM |
| 65 nM |
IC 50
2 nm, 142 nm, 65 nm, 1 nm, and 110 nm for p110α, p110β, p110γ, p110δ, and vps34, respectively.
References
[1] walls m, baxi sm, mehta pp, liu kk, zhu j, estrella h, li c, zientek m, zong q, smeal t, yin mj. targeting small cell lung cancer harboring pik3ca mutation with a selective oral pi3k inhibitor pf-4989216. clin cancer res. 2014 feb 1;20(3):631-43.
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