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IPN-60090

Product Name
IPN-60090
CAS No.
1853164-83-6
Chemical Name
IPN-60090
Synonyms
IACS-6274;GLS1-IN-1;IPN-60090;IACS-006274;IPN60090,IPN-60090;IACS-6274(IPN60090);IPN-60090 ( IACS-6274);IPN60090, 10 mM in DMSO;1-[(2R)-4-[6-[[2-[4-(3,3-difluorocyclobutoxy)-6-methyl-2-pyridyl]acetyl]amino]pyridazin-3-yl]-2-fluoro-butyl]-N-methyl-triazole-4-carboxamide;2-Pyridineacetamide, 4-[(3,3-difluorocyclobutyl)oxy]-N-[6-[(3R)-3-fluoro-4-[4-[(methylamino)carbonyl]-1H-1,2,3-triazol-1-yl]butyl]-3-pyridazinyl]-6-methyl-
CBNumber
CB77244426
Molecular Formula
C24H27F3N8O3
Formula Weight
532.52
MOL File
1853164-83-6.mol
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IPN-60090 Property

Density 
1.47±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 31.43 mg/mL (59.02 mM; Need ultrasonic)
pka
11.74±0.70(Predicted)
form 
Solid
color 
Pink to red
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0030361
Product name
IPN60090
Purity
99.14%
Packaging
5mg
Price
$580
Updated
2021/12/16
ChemScene
Product number
CS-0030361
Product name
IPN60090
Purity
99.14%
Packaging
10mg
Price
$980
Updated
2021/12/16
ChemScene
Product number
CS-0030361
Product name
IPN60090
Purity
99.14%
Packaging
25mg
Price
$1900
Updated
2021/12/16
ChemScene
Product number
CS-0030361
Product name
IPN60090
Purity
99.14%
Packaging
50mg
Price
$3200
Updated
2021/12/16
ChemScene
Product number
CS-0030361
Product name
IPN60090
Purity
99.14%
Packaging
100mg
Price
$5000
Updated
2021/12/16
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IPN-60090 Chemical Properties,Usage,Production

Uses

IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 can be used for solid tumors research, such as lung and ovarian cancers[1][2].

in vivo

IPN60090 (3 mg/kg for i.v.; 10 mg/kg for p.o.) has excellent pharmacokinetic properties, with CL=4.1 mL/min/kg, t1/2=1 hour, Cmax=19 μM, F%=89%[2].
IPN-60090 (oral administration; 100 mg/kg; twice daily; 30 days) shows similar efficacy and target engagement to CB-839 (HY-12248) dosed orally at 250 mg/kg twice daily. And the 100 mg/kg BID dose of IPN-60090 is a tolerated dose for the following model study[2].IPN-60090 (oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228 (HY-13328)) causes tumor growth inhibition. IPN-60090 alone demonstrates robust in vivo target engagement in a dose-dependent manner. The glutamate/glutamine ratios and the free plasma concentrations of IPN-60090 at 4 hours post-dose on both day 4 and day 28 are all decreased[2]. Furthermore, IPN-60090 in combination with TAK228 strongly causes an 85% tumor growth inhibition, IPN-60090 alone causes a 28% tumor growth inhibition in vivo[2].

Animal Model:Female CD-1 mice[2]
Dosage:3 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:Intravenous injection and oral administration
Result:CL (4.1 mL/min/kg), t1/2 (1 hour) for i.v.; Cmax (19 μM), F% (89%) for p.o..
Animal Model:Ru337 non-small cell lung cancer patient-derived xenograft (PDX) subcutaneous mouse model as monotherapy or in combination[2]
Dosage:100 mg/kg
Administration:Oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228
Result:Exhibited an improvement in the combination regimen group over either single agent.

References

[1] Maria Emilia Di Francesco, et al. Gls1 inhibitors for treating disease. WO2016004404A2.
[2] Michael J Soth, et al. Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem. 2020 Nov 12;63(21):12957-12977. DOI:10.1021/acs.jmedchem.0c01398

IPN-60090 Preparation Products And Raw materials

Raw materials

Preparation Products

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IPN-60090 Suppliers

China 28 United States 3 Global 31
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185;
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32470
Advantage
58
Chunchuang (Wuhan) Technology Co., Ltd
Tel
15727060112
Email
yutianchun2007@126.com
Country
China
ProdList
9811
Advantage
58
Wuhan Topule
Tel
+86-02787215551 +86-19945035818
Fax
027-87215551
Email
2936752263@qq.com
Country
China
ProdList
7988
Advantage
58
Hubei Kele Fine Chemical Co., Ltd
Tel
027-59101668 19945030958
Fax
027-59101668
Email
2881924765@qq.com
Country
China
ProdList
7933
Advantage
58
Kaifeng Mingren Pharmaceutical Co.,LTD
Tel
0371-65741762
Fax
QQ：2860768577
Email
sales@hasunny.com
Country
China
ProdList
2380
Advantage
58
InvivoChem
Tel
13549236410
Email
sales@invivochem.cn
Country
China
ProdList
6753
Advantage
58
Wuhan Shanhai Zhihe Biotechnology Co., Ltd.
Tel
17771424646
Email
shoubull@126.com
Country
China
ProdList
953
Advantage
58
TargetMol Chemicals Inc.
Tel
4008200310
Email
marketing@tsbiochem.com
Country
China
ProdList
24961
Advantage
58
Shanghai Yiyan Biotechnology Co. , Ltd.
Tel
021-69985186 13611928337
Email
3427709316@qq.com
Country
China
ProdList
7982
Advantage
58

1853164-83-6, IPN-60090Related Search:


  • IPN-60090
  • GLS1-IN-1
  • IACS-6274(IPN60090)
  • IPN-60090 ( IACS-6274)
  • IPN60090,IPN-60090
  • 1-[(2R)-4-[6-[[2-[4-(3,3-difluorocyclobutoxy)-6-methyl-2-pyridyl]acetyl]amino]pyridazin-3-yl]-2-fluoro-butyl]-N-methyl-triazole-4-carboxamide
  • 2-Pyridineacetamide, 4-[(3,3-difluorocyclobutyl)oxy]-N-[6-[(3R)-3-fluoro-4-[4-[(methylamino)carbonyl]-1H-1,2,3-triazol-1-yl]butyl]-3-pyridazinyl]-6-methyl-
  • IACS-6274
  • IPN60090, 10 mM in DMSO
  • IACS-006274
  • 1853164-83-6
  • APIs