CSF1R-IN-2
CSF1R-IN-2 Basic information
- Product Name:
- CSF1R-IN-2
- Synonyms:
-
- CSF1R-IN-2
- CSF1R inhibitor 2
- 1,15-Etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecine-12-carbonitrile, 3-amino-14-ethyl-11-fluoro-4,5,6,7,13,14-hexahydro-7-methyl-4-oxo-, (7S)-
- TPX-0022
- TPX-0022(CSF1R-IN-2)
- Elzovantinib (TPX-0022)
- colony stimulating factor 1 receptor,CSF-1R,CSF1R IN 2,inhibit,CSF1RIN2,c-Met/HGFR,CSF1R,CSF-1R-IN-2,Inhibitor,CSF-1 receptor,Src,c-Fms
- Elzovantinib
- CAS:
- 2271119-26-5
- MF:
- C20H20FN7O2
- MW:
- 409.42
- Mol File:
- 2271119-26-5.mol
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CSF1R-IN-2 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 25 mg/mL (61.06 mM; Need ultrasonic)
- form
- A solid
- color
- White to off-white
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CSF1R-IN-2 Usage And Synthesis
Uses
Elzovantinib (TPX-0022) 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].
in vivo
Elzovantinib (TPX-0022; 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].
Elzovantinib (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].
Elzovantinib 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. |
References
[1] WO 2019023417 A1.
CSF1R-IN-2Supplier
ShangHai Caerulum Pharma Discovery Co., Ltd.
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- 18149758185
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Shanghai Lollane Biological Technology Co.,Ltd.
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- 021-52996696，15000506266 15000506266
ShangHai Biochempartner Co.,Ltd
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- 177-54423994 17754423994
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Shanghai Rechem science Co., Ltd.
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- 021-31433387 15618786686
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Shanghai Yunpun industrial Co.,Ltd
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- 21-61726900 15202122459
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