JTE-952
Based on 1 Customer Validation
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 1255303-54-8
- Formula: C30H34N2O6
- Molecular Weight:518.60
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
IC50: 13 nM (CSF1R), 261 nM (TrkA)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of full-length human N-terminal His6-tagged IKKbeta expressed in baculovirus infected Sf21 insect cells using IKKtide as substrate
Inhibition of full-length human N-terminal His6-tagged IKKbeta expressed in baculovirus infected Sf21 insect cells using IKKtide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of full-length human N-terminal His6-tagged JNK3 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
Inhibition of full-length human N-terminal His6-tagged JNK3 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of full-length human N-terminal His6-tagged LCK expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate
Inhibition of full-length human N-terminal His6-tagged LCK expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of full-length human N-terminal His6-tagged LYN expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of full-length human N-terminal His6-tagged LYN expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin A expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin A expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full length His6-tagged CK2alpha expressed in baculovirus infected Sf21 insect cells using Casein Kinase 2 substrate peptide
Inhibition of human full length His6-tagged CK2alpha expressed in baculovirus infected Sf21 insect cells using Casein Kinase 2 substrate peptide
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full length N-terminal GST-tagged CHK1 expressed in baculovirus infected Sf21 insect cells using CHKtide as substrate
Inhibition of human full length N-terminal GST-tagged CHK1 expressed in baculovirus infected Sf21 insect cells using CHKtide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length C-terminal His6-tagged ZAP70 expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human full-length C-terminal His6-tagged ZAP70 expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal GST-tagged SAPK2a expressed in baculovirus infected Sf21 insect cells using MBP as substrate
Inhibition of human full-length N-terminal GST-tagged SAPK2a expressed in baculovirus infected Sf21 insect cells using MBP as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal GST-tagged SAPK2b2 expressed in baculovirus infected Sf21 insect cells using MBP as substrate
Inhibition of human full-length N-terminal GST-tagged SAPK2b2 expressed in baculovirus infected Sf21 insect cells using MBP as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His6-tagged Fyn expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate
Inhibition of human full-length N-terminal His6-tagged Fyn expressed in baculovirus infected Sf21 insect cells using Src peptide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His6-tagged PKBalpha expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate
Inhibition of human full-length N-terminal His6-tagged PKBalpha expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His6-tagged PKCalpha expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
Inhibition of human full-length N-terminal His6-tagged PKCalpha expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His6-tagged PKCgamma expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
Inhibition of human full-length N-terminal His6-tagged PKCgamma expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His-tagged p70S6K expressed in baculovirus infected Sf21 insect cells using CKRRRLASLR as substrate
Inhibition of human full-length N-terminal His-tagged p70S6K expressed in baculovirus infected Sf21 insect cells using CKRRRLASLR as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged c-kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal GST-tagged c-kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged EGFR (696 to end residues) expressed in baculovirus infected Sf21 insect cells using Angiotensin II peptide as substrate
Inhibition of human N-terminal GST-tagged EGFR (696 to end residues) expressed in baculovirus infected Sf21 insect cells using Angiotensin II peptide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged FGFR1 (456 to 765 residues) expressed in baculovirus infected Sf21 insect cells using IGF-IRtide (12-527) as substrate
Inhibition of human N-terminal GST-tagged FGFR1 (456 to 765 residues) expressed in baculovirus infected Sf21 insect cells using IGF-IRtide (12-527) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged Flt1 (783 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
Inhibition of human N-terminal GST-tagged Flt1 (783 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged Flt3 (564 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
Inhibition of human N-terminal GST-tagged Flt3 (564 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged SGK1 (61 to 431 residues) expressed in baculovirus infected Sf21 insect cells Akt/SGK peptide as substrate
Inhibition of human N-terminal GST-tagged SGK1 (61 to 431 residues) expressed in baculovirus infected Sf21 insect cells Akt/SGK peptide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged (11 to 552 residues) ROCK2 expressed in baculovirus infected Sf21 insect cells using Long S6 Kinase as substrate
Inhibition of human N-terminal His6-tagged (11 to 552 residues) ROCK2 expressed in baculovirus infected Sf21 insect cells using Long S6 Kinase as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged (2 to end residues) PKCbeta expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
Inhibition of human N-terminal His6-tagged (2 to end residues) PKCbeta expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged FGFR3 (447 to 761 residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal His6-tagged FGFR3 (447 to 761 residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 insect cells using phosphoglycogen synthase peptide-2 as substrate
Inhibition of human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 insect cells using phosphoglycogen synthase peptide-2 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged IGF1R (959 to end residues) expressed in baculovirus infected Sf21 insect cells
Inhibition of human N-terminal His6-tagged IGF1R (959 to end residues) expressed in baculovirus infected Sf21 insect cells
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged insulin receptor (1005 to 1310 residues) expressed in baculovirus infected Sf21 insect cells
Inhibition of human N-terminal His6-tagged insulin receptor (1005 to 1310 residues) expressed in baculovirus infected Sf21 insect cells
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged MET (974 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
Inhibition of human N-terminal His6-tagged MET (974 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged MSK1 (2 to end residues) expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate
Inhibition of human N-terminal His6-tagged MSK1 (2 to end residues) expressed in baculovirus infected Sf21 insect cells using Crosstide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged PDGFRalpha (550 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal His6-tagged PDGFRalpha (550 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged PDGFRbeta (557 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal His6-tagged PDGFRbeta (557 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged PDK1 (52 to end residues) expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate
Inhibition of human N-terminal His6-tagged PDK1 (52 to end residues) expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged PLK1 expressed in baculovirus infected Sf21 insect cells
Inhibition of human N-terminal His6-tagged PLK1 expressed in baculovirus infected Sf21 insect cells
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged SYK expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal His6-tagged SYK expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His6-tagged TIE2 (771 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
Inhibition of human N-terminal His6-tagged TIE2 (771 to end residues) expressed in baculovirus infected Sf21 insect cells using Poly (Glu4-Tyr) (4:1) as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His-tagged JNK1alpha1 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
Inhibition of human N-terminal His-tagged JNK1alpha1 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal His-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells using myelin basic protein as substrate
Inhibition of human N-terminal His-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells using myelin basic protein as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of recombinant full-length human N-terminal GST-tagged CDK1/cyclinB expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
Inhibition of recombinant full-length human N-terminal GST-tagged CDK1/cyclinB expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of recombinant full-length human N-terminal His6-tagged AuroraA expressed in baculovirus infected Sf21 insect cells using Kemptide as substrate
Inhibition of recombinant full-length human N-terminal His6-tagged AuroraA expressed in baculovirus infected Sf21 insect cells using Kemptide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of recombinant human N-terminal His6-tagged Abl (27 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
Inhibition of recombinant human N-terminal His6-tagged Abl (27 to end residues) expressed in baculovirus infected Sf21 insect cells using Abltide as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
261 nM
Compound: JTE-952; (S)-8b
|
Inhibition of recombinant human N-terminal His6-tagged TrkA (440 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
Inhibition of recombinant human N-terminal His6-tagged TrkA (440 to end residues) expressed in baculovirus infected Sf21 insect cells using KKKSPGEYVNIEFG as substrate
|
[PMID: 30755337] |
| Sf21 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of full-length human N-terminal His-tagged JNK2alpha2 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
Inhibition of full-length human N-terminal His-tagged JNK2alpha2 expressed in baculovirus infected Sf21 insect cells using ATF2 as substrate
|
[PMID: 30755337] |
| Sf9 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human full-length N-terminal His-tagged SRC expressed in baculovirus infected Sf9 insect cells using Poly-(Glu4:Tyr) as substrate measured after 35 mins
Inhibition of human full-length N-terminal His-tagged SRC expressed in baculovirus infected Sf9 insect cells using Poly-(Glu4:Tyr) as substrate measured after 35 mins
|
[PMID: 30755337] |
| Sf9 | IC50 |
>1000 nM
Compound: JTE-952; (S)-8b
|
Inhibition of human N-terminal GST-tagged c-RAF Y340D/Y341D double mutant (306 to 648 residues) expressed in baculovirus infected Sf9 insect cells using MEK1(K97R) as substrate measured after 1 hr
Inhibition of human N-terminal GST-tagged c-RAF Y340D/Y341D double mutant (306 to 648 residues) expressed in baculovirus infected Sf9 insect cells using MEK1(K97R) as substrate measured after 1 hr
|
[PMID: 30755337] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mouse model of collagen-induced arthritis (CIA model)[1].
-
Dosage:3 mg/kg.
-
Administration:Oral once-daily.
-
Result:Reduced the overall progression of the clinical score, including inflammation and bone erosion.
Chemical Information
-
CAS No. 1255303-54-8
-
Appearance Solid
-
Molecular Weight 518.60
-
Formula C30H34N2O6
-
Color White to off-white
-
SMILES
O=C(N1CC(C2=CC=C(OCC3=CC=C(C4CC4)C=C3)C(OC)=C2)C1)C5=NC=CC(COC[C@@H](O)CO)=C5
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (192.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (269 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9283 mL | 9.6413 mL | 19.2827 mL | 48.2067 mL |
| 5 mM | 0.3857 mL | 1.9283 mL | 3.8565 mL | 9.6413 mL | |
| 10 mM | 0.1928 mL | 0.9641 mL | 1.9283 mL | 4.8207 mL | |
| 15 mM | 0.1286 mL | 0.6428 mL | 1.2855 mL | 3.2138 mL | |
| 20 mM | 0.0964 mL | 0.4821 mL | 0.9641 mL | 2.4103 mL | |
| 25 mM | 0.0771 mL | 0.3857 mL | 0.7713 mL | 1.9283 mL | |
| 30 mM | 0.0643 mL | 0.3214 mL | 0.6428 mL | 1.6069 mL | |
| 40 mM | 0.0482 mL | 0.2410 mL | 0.4821 mL | 1.2052 mL | |
| 50 mM | 0.0386 mL | 0.1928 mL | 0.3857 mL | 0.9641 mL | |
| 60 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8034 mL | |
| 80 mM | 0.0241 mL | 0.1205 mL | 0.2410 mL | 0.6026 mL | |
| 100 mM | 0.0193 mL | 0.0964 mL | 0.1928 mL | 0.4821 mL |