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N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide structure

CAS No:
850879-09-3
Formula:
C23H21N5O3S
Chemical Name:
N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide
Synonyms:
N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide;1-Piperazinecarbothioamide, N-(1,3-benzodioxol-5-ylmethyl)-4-benzofuro(3,2-D)pyrimidin-4-yl-;Mp470;AMuvatinib;HPK 56;MP-470(MP 470);AMuvatinib (MP-470);AMuvatinib (MP-470, HPK 56)
Categories:
Biochemical Engineering > Inhibitors

Description

Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.IC50 Value: 10 nM(c-KitD816H); 40 nM(PDGFRαV561D); 81 nM(Flt3D835Y) [1]Target: c-Kit; PDGFRα; FLT3in vitro: The hydrochloride salt of MP-470 also inhibits several mutants of c-Kit, including c-KitD816V, c-KitD816H, c-KitV560G, and c-KitV654A, as well as a Flt3 mutant (Flt3D835Y) and two PDGFRα mutants (PDGFRαV561D and PDGFRαD842V), with IC50 of 10 nM to

N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide Basic Attributes

Molecular Weight：

447.51

Exact Mass：

447.136505

Characteristics

PSA：

108

XLogP3：

3.5

Density：

1.4±0.1 g/cm3

Boiling Point：

649.5±65.0°C at 760 mmHg

Flash Point：

346.6±34.3 °C

Refractive Index：

1.739

N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide Use and Manufacturing

Methods of Manufacturing

4-Benzo[4, 5]furo[3, 2-d]pyrimidin-4-yl-piperazine-1-carbothioic acid (benzof1, 31dioxol-5-ylmethvl)-amide (3) To a solution of 4-piperazinobenzofurano [3, 2-d] pyrimidine (200 mg, 0.79 mmol) and pyridine (0.5 mL, 7.9 mmol) in dichloromethane (20 mL) was added a solution of product 1c in dichloromethane (20mL) and this was stirred overnight. Methanol was added to quench excess thiophosgene, and the residue after removal of solvent was purified by silica gel column chromatography eluting with 5percent methanol/dichloromethane and further recrystallized from dichloromethane/hexane to give 150 mg (37percent). HNMR (CDCl3, 300MHZ) a 4.09 (s, 4H), 4.27 (s, 4H), 4.82 (d, J = 4.7Hz, 2H), 5.99 (s, 2H), 6.77-6. 79 (m, 1 H), 6.80-6. 83 (m, 1H), 6.89 (s, 1 H), 7.47-7. 52 (m, 1 H), 7.61-7. 65 (m, 1 H), 7.66-7. 70 (m, 1 H), 8.33 (d, J = 7. 0Hz, 1 H). FAB HRMS [M+H] + calcd for C23H21N503S : 447.1365 ; found 448. 1443. Combustion Analysis: C23H21N5O3S Requires C 61.73percent, H 4.73percent, N 15.65percent, O 10.73percent, S 7.17percent ; Found C 61. 95percent, H 4.99percent, N 15.93percent, 0 11. 13percent, S 7. 55percent.

Uses

MP-470 (Amuvatinib) is a potent and multi-targeted inhibitor of c-KitD816H, PDGFαV561D and Flt3D835Y with IC50 of 10 nM, 40 nM and 81 nM, respectively.

Recommended Suppliers of N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

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N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

CAS No.: 850879-09-3

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Amuvatinib(MP-470)

CAS No.: 850879-09-3

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Guide of N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

Description
Basic Attributes
Characteristics
Use and Manufacturing
Recommended Suppliers
Latest News
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N-(1,3-Benzodioxol-5-ylmethyl)-4-benzofuro[3,2-d]pyrimidin-4-yl-1-piperazinecarbothioamide

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