[CAS NO. 1644545-52-7]  Vorasidenib (AG-881)

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PRODUCTS SPECIFICATIONS [1644545-52-7]

Store
Catalog
SLK-S8611
Brand
Selleck
CAS
1644545-52-7

DESCRIPTION [1644545-52-7]

Overview

MDLMFCD31630835
Molecular Weight414.74
Molecular FormulaC14H13ClF6N6
SMILESC[C@@H](NC1=NC(C2=NC(Cl)=CC=C2)=NC(N[C@H](C)C(F)(F)F)=N1)C(F)(F)F

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.4111 mL12.0557 mL24.1115 mL
5 mM0.4822 mL2.4111 mL4.8223 mL
10 mM0.2411 mL1.2056 mL2.4111 mL
50 mM0.0482 mL0.2411 mL0.4822 mL

Description

Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both .

Targets

IDH1 [1]IDH2 [1]

In vitro

Pan-IDH1/2 inhibitor (AG881) selectively inhibit mutant IDH protein and induce cell differentiation in in vitro and in vivo models. Upon administration, pan-IDH mutant inhibitor AG-881 specifically inhibits mutant forms of IDH1 and IDH2, thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH mutations.

In vivo

AG-881 fully penetrates the blood-brain barrier. AG-881 has been developed and is in early phase I testing for patients with IDH mutation-positive hematologic malignancies and solid tumors, including glioma.