| Identification | Back Directory | [Name]
IPN-60090 | [CAS]
1853164-83-6 | [Synonyms]
IPN-60090
GLS1-IN-1
IPN60090,IPN-60090
IACS-6274(IPN60090)
IPN-60090 ( IACS-6274) | [Molecular Formula]
C24H27F3N8O3 | [MDL Number]
MFCD33023198 | [MOL File]
1853164-83-6.mol | [Molecular Weight]
532.52 |
| Chemical Properties | Back Directory | [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) | [form ]
Solid | [pka]
11.74±0.70(Predicted) | [color ]
Pink to red |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
Wuhan Topule
|
| Tel: |
+86-02787215551 +86-19945035818 |
| Website: |
http://www.topule.com/ |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|