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Sulfatinib

Catalog No. T4075 CAS 1308672-74-3

Synonyms: KDR-IN-1

Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.

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Sulfatinib, CAS 1308672-74-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 159.00
50 mg	In stock	$ 239.00
100 mg	In stock	$ 372.00
1 mL * 10 mM (in DMSO)	In stock	$ 76.00

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Purity: 100%

Purity: 98.93%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.
In vitro	Sulfatinib inhibits VEGFR1, 2, and 3, FGFR1 and CSF1R kinases with IC 50 s in a range of 1 to 24 nM. Sulfatinib strongly blocks VEGF induced VEGFR2 phosphorylation in HEK293KDR cells and CSF1 stimulated CSF1R phosphorylation in RAW264.7 cells with IC 50 of 2 and 79 nM, respectively. Sulfatinib also attenuates VEGF or FGF stimulated HUVEC cells proliferation with IC 50 < 50 nM [1]. Also, it is a hERG inhibitor with IC 50 of 6.8 μM in CHO cell [2].
In vivo	In animal studies, a single oral dose of Sulfatinib effectively inhibits VEGFR2 phosphorylation stimulated by VEGF in lung tissues of nude mice in an exposure-dependent manner. Additionally, a rise in FGF23 plasma levels 24 hours after dosing indicates a suppression of FGFR signaling. Sulfatinib exhibits strong antitumor efficacy across various human xenograft models and significantly reduces CD31 expression, which evidences its potent antiangiogenic effects via the inhibition of VEGFR and FGFR signaling pathways. In the CT-26 syngeneic murine colon cancer model, Sulfatinib achieves moderate tumor growth inhibition following monotherapy. Moreover, after a 10 mg/kg oral dose, the AUC and C_max in mice are 397 ng/mL and 138 ng/mL, respectively [1].

Synonyms	KDR-IN-1
Molecular Weight	480.58
Formula	C24H28N6O3S
CAS No.	1308672-74-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL

References and Literature

1. PCT Int. Appl. (2011), WO 2011060746 A1 20110526.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Drug Repurposing Compound Library Tyrosine Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Anti-Ovarian Cancer Compound Library Anti-Breast Cancer Compound Library

Related Products

Related compounds with same targets

VEGFR-2-IN-31 Dovitinib lactate SCR-1481B1 PD173074 Riddelline ODM-203 SU14813 TAK-593

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Sulfatinib 1308672-74-3 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors HER VEGFR FGFR KDR-IN-1 inhibitor inhibit

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