What is the Regorafenib?

Regorafenib is , while it's Molecular Formula is C21H15ClF4N4O3. Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively

What is the CAS number for Regorafenib?

The CAS number of Regorafenib is 755037-03-7.

What is Regorafenib (755037-03-7) used for?

Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity. It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectivey) as well as other kinases. In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models. It also reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models. Formulations containing regorafenib have been used in the treatment of advanced gastrointestinal stromal tumors and metastatic colorectal cancer.

What is the Regorafenib?

Regorafenib is , while it's Molecular Formula is C21H15ClF4N4O3. Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively

What is the CAS number for Regorafenib?

The CAS number of Regorafenib is 755037-03-7.

What is Regorafenib (755037-03-7) used for?

Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity. It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectivey) as well as other kinases. In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models. It also reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models. Formulations containing regorafenib have been used in the treatment of advanced gastrointestinal stromal tumors and metastatic colorectal cancer.

Product classification

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755037-03-7

Product Name:Regorafenib
Molecular Formula:C₂₁H₁₅ClF₄N₄O₃
Molecular Weight:482.822

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Product Details

pd_meltingpoint:206.0 to 210.0 °C

Purity:99%

High Quality Chinese Factory supply 755037-03-7 Regorafenib

Molecular Formula:C21H15ClF4N4O3
Molecular Weight:482.822
Melting Point:206.0 to 210.0 °C
Boiling Point:513.4 °C at 760 mmHg
PKA:12.04±0.70(Predicted)
Flash Point:264.3 °C
PSA：92.35000
Density:1.491 g/cm³
LogP:6.22570

755037-03-7 Relevant articles

Synthesis method of regorafenib

-

Paragraph 0029-0031, (2021/04/21)

The invention provides a synthesis metho...

Interrupted aza-Wittig reactions using iminophosphoranes to synthesize 11C-carbonyls

Ismailani, Uzair S.,Munch, Maxime,Mair, Braeden A.,Rotstein, Benjamin H.

supporting information, p. 5266 - 5269 (2021/06/06)

A direct CO2-fixation methodology couple...

Preparation method of regorafenib

-

Paragraph 0025-0040, (2021/05/29)

The invention relates to a preparation m...

Regorafenib analogues and their ferrocenic counterparts: Synthesis and biological evaluation

Wilde, Myron,Arzur, Danielle,Baratte, Blandine,Lefebvre, Dorian,Robert, Thomas,Roisnel, Thierry,Le Jossic-Corcos, Catherine,Bach, Stéphane,Corcos, Laurent,Erb, William

supporting information, p. 19723 - 19733 (2020/12/04)

Approved by the FDA in 2012, regorafenib...

755037-03-7 Process route

: 757251-39-1
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

: 327-78-6
4-chloro-3-(trifluoromethyl)phenyl isocyanate

: 755037-03-7
regorafenib

Conditions

Conditions	Yield
In ethyl acetate; at 20 ℃; for 1.5h;	94.5%
In dichloromethane; at 0 - 20 ℃; for 16h; Inert atmosphere;	90%
In dichloromethane; for 24h;	87%
In acetone; at 40 ℃; for 5h;	85%
In tetrahydrofuran; toluene; at 27 ℃; for 4.5h;	74.9%
In tetrahydrofuran; at 30 ℃; for 12h;	73.46%
In dichloromethane; at 0 - 25 ℃; for 3h;	67.2%
In toluene; at 20 ℃; for 72h;	47%
In toluene; at 20 ℃; for 72h;	47%
In toluene; at 20 ℃; for 72h;	47%
In toluene; at 20 ℃; for 72h;	47%
In toluene; at 20 ℃; for 72h;	47%
In ethyl acetate; at 20 - 45 ℃; for 1.5h;
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; In tetrahydrofuran; toluene; at 20 ℃; for 4.5h; With acetyl chloride; In tetrahydrofuran; methanol; toluene; for 2.25h;
In dichloromethane; at 0 - 5 ℃; for 4h; Inert atmosphere;	350 g
In acetone; at 25 - 30 ℃;	5.5 g
In ethyl acetate; at 20 ℃; for 0.5h;
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; In tetrahydrofuran; at 25 ℃; for 4h; Inert atmosphere; With hydrogenchloride; In water; at 25 ℃; for 4h;
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; In dichloromethane; at 25 - 30 ℃; Inert atmosphere; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; In dichloromethane; at 0 - 30 ℃;
In tetrahydrofuran; at 20 ℃; for 5h;	86.7 g
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide; 4-chloro-3-(trifluoromethyl)phenyl isocyanate; With acetic acid; In tetrahydrofuran; toluene; at 20 ℃; for 4.5h; With acetyl chloride; In tetrahydrofuran; methanol; for 2.25h; With water; sodium hydroxide; In acetone; at 40 ℃; for 0.5h;	31.5 g
In dichloromethane; ethyl acetate; at 20 ℃; for 18h; Inert atmosphere; Schlenk technique;	169 mg

: 757251-39-1
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

: 42558-54-3
Methyl 4-methyl-3-oxopentanoate

: 320-51-4
4-chloro-3-trifluoromethyl-aniline

: 755037-03-7
regorafenib

Conditions

Conditions	Yield
With dmap; In N,N-dimethyl-formamide; at 140 ℃; for 4h; Temperature; Green chemistry;	96.8%

755037-03-7 Upstream products

757251-39-1
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide
327-78-6
4-chloro-3-(trifluoromethyl)phenyl isocyanate
399-95-1
4-amino-3-fluorophenol
1338722-52-3
C₁₂H₁₆FNO

755037-03-7 Downstream products

835621-08-4
4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide mesylate
835621-09-5
4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide phenylsulfonate
835621-07-3
4-{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide hydrochloride
757251-39-1
4-(4-amino-3-fluorophenoxy)pyridine-2-carboxylic acid methyl amide

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