ChemicalBook > CAS DataBase List > PF-4989216

PF-4989216

Product Name
PF-4989216
CAS No.
1276553-09-3
Chemical Name
PF-4989216
Synonyms
CS-1547;PF-4989216;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
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PF-4989216 Property

storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
crystalline solid
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19308
Product name
PF-4989216
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
19308
Product name
PF-4989216
Purity
≥98%
Packaging
5mg
Price
$172
Updated
2024/03/01
Cayman Chemical
Product number
19308
Product name
PF-4989216
Purity
≥98%
Packaging
10mg
Price
$299
Updated
2024/03/01
Cayman Chemical
Product number
19308
Product name
PF-4989216
Purity
≥98%
Packaging
25mg
Price
$533
Updated
2024/03/01
ChemScene
Product number
CS-5205
Product name
PF-4989216
Purity
99.43%
Packaging
50mg
Price
$696
Updated
2021/12/16
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PF-4989216 Chemical Properties,Usage,Production

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

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> p110γ
(Cell-free assay)
TargetValue
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.

PF-4989216 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-4989216 Suppliers

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1276553-09-3, PF-4989216Related Search:

Morpholinazole Diphenhydramine Morpholine TRIS(PENTAFLUOROPHENYL)PHOSPHINE 2-FLUOROPHENYL CYCLOPENTYL KETONE

  • CS-1547
  • PF-4989216;PF 4989216;PF4989216
  • PF-4989216
  • 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)-
  • Apoptosis,inhibit,Phosphoinositide 3-kinase,PF4989216,PF-4989216,PI3K,Inhibitor
  • 1276553-09-3