Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  API >  Antineoplastic agents >  Tinib Antineoplastic drugs >  Savolitinib

Savolitinib

Basic information Safety Supplier Related

Savolitinib Basic information

Product Name:
Savolitinib
Synonyms:
  • AZD6094,Volitinib, HMPL-504, Savolitinib
  • 1-[(1S)-1-Imidazo[1,2-a]pyridin-6-ylethyl]-6-(1-methyl-1H-pyrazol-4-yl)-1H-1,2,3-triazolo[4,5-b]pyrazine
  • (S)-1-(1-(imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine
  • Volitinib
  • Savolitinib
  • HMPL-504(AZD6094, Volitinib)
  • EOS-60799
  • AZD-6094)
CAS:
1313725-88-0
MF:
C17H15N9
MW:
345.36
Product Categories:
  • API
Mol File:
1313725-88-0.mol
More
Less

Savolitinib Chemical Properties

Melting point:
205-207°C
Density 
1.55±0.1 g/cm3(Predicted)
storage temp. 
-20°C Freezer
solubility 
DMSO (Slightly), Methanol (Slightly)
pka
5.67±0.50(Predicted)
form 
Solid
color 
Pale Beige
InChI
InChI=1S/C17H15N9/c1-11(12-3-4-15-18-5-6-25(15)10-12)26-17-16(22-23-26)19-8-14(21-17)13-7-20-24(2)9-13/h3-11H,1-2H3/t11-/m0/s1
InChIKey
XYDNMOZJKOGZLS-NSHDSACASA-N
SMILES
C12N=NN([C@H](C3=CN4C=CN=C4C=C3)C)C1=NC(C1=CN(C)N=C1)=CN=2
CAS DataBase Reference
1313725-88-0
More
Less

Savolitinib Usage And Synthesis

Description

Savolitinib selectively inhibits the MET receptor, blocking the PI3K/AKT/MAPK-signaling pathway as well as downregulating MYC.

Uses

Savolitinib is a potent and highly selective c-Met inhibitor. Savoltinib demonstrated anti-tumor efficacy in a panel of cMet-dysregulated gastric cancer PDX models. Savolitinib also demonstrated good antitmuor activities.

Clinical Use

It is currently being evaluated in phase I clinical trials in combination with EGFR TKIs in NSCLC patients.

Synthesis

The synthesis of savolitinib started with 6-amino-3-carboxypyridine (20.1), which was treated with chloroacetaldehyde to generate the imidazopyridine 20.2. The carboxylic acid was converted to the Weinreb amide 20.3 and treated with methylmagnesium bromide to give the methyl ketone 20.4. The ketone was converted to the chiral amine 20.5 using a commercially available aminotransferase with the cofactors pyridoxal phosphate and isopropylamine as a nitrogen source. After process workup, the amine was isolated as the dihydrochloride salt (20.5). The free base was obtained by treatment with alkaline conditions, which was subsequently reacted with commercially available 3,5-dibromopyrazin-2-amine (20.6) to give the secondary amine 20.7. Next, nitrosyl ion formation and cyclization gave the 1,2,3-triazole 20.8. Finally, Suzuki coupling with 20.9 completed the construction of savolitinib (20). The boronic acid ester 20.9 was obtained from 4-bromo-1-methyl-1H-pyrazole by lithium-halogen exchange and workup with triisopropylborate quenching.

in vivo

Savolitinib (Compound 28; 1-10.0 mg/kg; oral administration; daily; for 21 days; athymic nude mice) demonstrates dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model. In addition, none of the mice in the dosing groups exhibits body weight loss during the experiment[1].

Animal Model:U87MG xenograft model in athymic nude mice[1]
Dosage:1 mg/kg, 2.5 mg/kg and 10.0 mg/kg
Administration:Oral administration; daily; for 21 days
Result:Demonstrated dose-dependent tumor growth inhibition in a U87MG subcutaneous xenograft model.

SavolitinibSupplier

DKMbiochem.Co. Ltd Gold
Tel
15901859516
Email
sales@DKMbiochem.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
ChengDu TongChuangYuan Pharmaceutical Co.Ltd
Tel
28-83379370 13880556291
Email
tcy@tcypharm.com
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Shanghai Hope Chem Co., Ltd.，
Tel
+21-18501659228 18501659228
Email
info@hope-chem.com
More
Less

Savolitinib(1313725-88-0)Related Product Information