Chemical Structure : HMPL-306
CAS No.:
2301974-60-5
HMPL-306
(Ranosidenib)
Catalog No.: PC-24264Not For Human Use, Lab Use Only.
HMPL-306 (Ranosidenib) is a potent, selective dual inhibitor of isocitrate dehydrogenase IDH1 and IDH2 with cell IC50 of 50/31/26 nM for U87MG IDH1-R132H/TF1 IDH1-R132H/ HT1080 (IDH1-R132C), respectively.
Bulk size, bulk discount!
Welcome credit card payment!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HMPL-306 (Ranosidenib) is a potent, selective dual inhibitor of isocitrate dehydrogenase IDH1 and IDH2 with cell IC50 of 50/31/26 nM for U87MG IDH1-R132H/TF1 IDH1-R132H/ HT1080 (IDH1-R132C), respectively.
HMPL-306 (Ranosidenib) shows excellent selectivity against SafetyScreen panel at CEREP.
HMPL-306 (Ranosidenib) at 25 mg/kg demonstrated robust and sustained 2-HG inhibition in tumors, with inhibitory rates reaching 96%, 98% and 93% at 16, 24, and 40 h post dosing, respectively.
HMPL-306 (Ranosidenib) also displayed potent and durable mutant IDH1 inhibitory activity in fibrosarcoma HT1080 model harboring IDH1 R132C mutation.
HMPL-306 (Ranosidenib) demonstrated better brain penetration in mice.
HMPL-306 (Ranosidenib) showed good PK and safety profiles and reduced 2-HG in vivo robustly and sustainably in the mutant IDH1 and 2 tumor xenograft models.
Physicochemical Properties
|
M.Wt
|
453.31
|
|
Formula
|
C15H16F9N5O
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
Shipping
|
|
|
Solubility
|
10 mM in DMSO
|
|
Chemical Name/SMILES
|
(S)-3-(4,6-bis(((R)-1,1,1-trifluoropropan-2-yl)amino)-1,3,5-triazin-2-yl)-2,6,6-trifluorocyclohex-2-en-1-ol
|
References
1. Xiao K, et al. ACS Med Chem Lett. 2025 Feb 13;16(3):454-463.
Contact Us
sales@probechem.com
