my account
Login
  Loading... Please wait...

Product Details

Sitravatinib | Multikinase inhibitor / Immuno-oncology agent

Sitravatinib (1123837-84-2) is a broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels.1 Sitravatinib has been tested in mouse models of sarcoma and showed better efficacy than both imatinib and crizotinib. Because of its unique kinase inhibition profile (especially that of TAM receptors), it has been used to restore response to anti-PD-1 therapy (nivolumab) in NSCLC patients.2 Sitravatinib was able to significantly alter the immunosuppressive tumor microenvironment in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.3

References/Citations

1) Parag et al. (2016) Significant blockade of multiple receptor kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma; Oncotarget 7 4093
2) Leal et al. (2017) Evidence of clinical activity of sitravatinib in combination with nivolumab in NSCLC patients progressing on prior checkpoint inhibitors; J. Thorac. Oncol. 12 S1803
3) Du et al. (2018); Sitravatinib potentiates immune checkpoint blockade in refractory cancer models; JCI Insight 3 124184

swipe
Image 1

Catalog#  10-4826-0005

$50.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
Request Bulk Quote
CAS:
1123837-84-2
Catalog Number:
10-4826
Activity:
Multikinase inhibitor / Immuno-oncology agent
Chemical Name:
1-N’-[3-Fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Alternate Names:
MGCD516
Molecular Weight:
629.68
Molecular Formula:
C33H29N5O4S
Solubility:
Soluble in DMSO (up to at least 25 mg/ml), or in Ethanol (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

Connect with Focus

Click the button below to add the Sitravatinib | Multikinase inhibitor / Immuno-oncology agent to your wish list.