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
color 
White to off-white
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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

Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
Deyang Yuehe Bio-Pharmaceutical Co.,Ltd
Tel
028-82729560 18030702676
Fax
028-82729560
Email
sales@yuehepharm.com
Country
China
ProdList
179
Advantage
58
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Fax
0512-87182056
Email
lingling.qi@yacoo.com.cn
Country
China
ProdList
7295
Advantage
60
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4512
Advantage
55

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


  • 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