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| Cas No.: | 2271119-26-5 |
| Chemical Name: | Csf1R-IN-2 |
| Synonyms: | CSF1R-IN-2;TPX0022;NSC820832;elzovantinib;TTY12Q00LY;Elzovantinib [INN];TPX002;GTPL11869;s9620;compound 5 [WO2019023417A1] |
| SMILES: | FC1C=CC2=C(C=1C#N)CN(CC)C1C=CN3C(=C(C(N)=N3)C(NC[C@H](C)O2)=O)N=1 |
| Formula: | C20H20FN7O2 |
| M.Wt: | 409.425 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively[1]. |
| Target: | IC50: 0.12 nM (SRC), 0.14 nM (MET), 0.76 nM (c-FMS)[1]. |
| In Vivo: | CSF1R-IN-2 (compound 5: p.o., BID, 13 days) treatment results in an 85% tumor regression and no body weight loss is observed after 21 days treatment in mice[1]. CSF1R-IN-2 (compound 5: p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively in SCID/Beige mice[1]. CSF1R-IN-2 (compound 5) inhibits MET activity in MKN-45 tumors following oral administration in mice[1]. Animal Model: Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model[1]. Dosage: 15 mg/kg. Administration: PO, BID (twice daily) for 13 days. Result: Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment. Animal Model: SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3[1]. Dosage: 5 and 15 mg/kg. Administration: PO, BID (twice daily) for 10 days. Result: Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively. |
| In Vitro: | CSF1R-IN-2 (compound 5) causes the suppression of MET autophosphorylation as well as the downstream STAT3, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines[1]. |
| References: | [1]. WO 2019023417 A1. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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| 2018-0101 |
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