GSK321 - CAS 1816331-63-1
Catalog number: 1816331-63-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C28H28FN5O3
Molecular Weight:
501.56
COA:
Inquire
Targets:
Isocitrate Dehydrogenase (IDH)
Description:
GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50= 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 stably decreased 2-hydroxyglutarate (2-HG) production in several different IDH1 mutant AML cells within a 2–3 week time frame ex vivo. Because of the allosteric nature of the interaction, GSK321 is able to inhibit multiple mutant forms of IDH1, which is consistent with our cell biological observations. Furthermore, GSK321 retains excellent potency in cells, since it does not compete with the tightly bound cofactor.
Purity:
>98%
Appearance:
Light yellow to yellow Solid
Synonyms:
(7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; (7R)-1-[(4-fluorophenyl)methyl]-N-[3-[(1S)-1-hydroxyethyl]phenyl]-7-methyl-5-(1H-pyrrole-2-carbonyl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-3-carboxamide; GSK321; GSK-321; BDBM195601
MSDS:
Inquire
InChIKey:
IVFDDVKCCBDPQZ-MSOLQXFVSA-N
InChI:
InChI=1S/C28H28FN5O3/c1-17-14-33(28(37)24-7-4-12-30-24)16-23-25(27(36)31-22-6-3-5-20(13-22)18(2)35)32-34(26(17)23)15-19-8-10-21(29)11-9-19/h3-13,17-18,30,35H,14-16H2,1-2H3,(H,31,36)/t17-,18+/m1/s1
Canonical SMILES:
CC1CN(CC2=C1N(N=C2C(=O)NC3=CC=CC(=C3)C(C)O)CC4=CC=C(C=C4)F)C(=O)C5=CC=CN5
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Isocitrate Dehydrogenase (IDH) Products


CAS 1355326-35-0 AGI-5198

AGI-5198
(CAS: 1355326-35-0)

AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.

CAS 1446502-11-9 Enasidenib

Enasidenib
(CAS: 1446502-11-9)

Enasidenib, aslo known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).

CAS 1816331-66-4 GSK864

GSK864
(CAS: 1816331-66-4)

GSK864 is a cell penetrant, selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant with IC50 values of 8.8, 15.2 and 16.6 nM for IDH1 mutant...

CAS 1432660-47-3 AGI-6780

AGI-6780
(CAS: 1432660-47-3)

AGI-6780 is an IDH2 inhibitor that potently and selectively inhibits the tumor-associated mutant IDH2/R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent agai...

AG-120
(CAS: 1448346-63-1)

AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.

CAS 1650550-25-6 Enasidenib mesylate

Enasidenib mesylate
(CAS: 1650550-25-6)

Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes indicated for the treatment of adult patients ...

CAS 1448347-49-6 Ivosidenib

Ivosidenib
(CAS: 1448347-49-6)

Ivosidenib is an oral inhibitor that specifically inhibits a mutated form of IDH1 in the cytoplasm, which blocks the proliferation of tumor cells expressing IDH...

CAS 1429180-08-4 SCHEMBL14831541

SCHEMBL14831541
(CAS: 1429180-08-4)

SCHEMBL14831541, also called as Mutant IDH1 inhibitor, is an inhibitor of mutant IDH1 which is key enzymes found in cellular metabolism.

CAS 1355326-21-4 Mutant IDH1-IN-1

Mutant IDH1-IN-1
(CAS: 1355326-21-4)

Mutant IDH1-IN-1, a mutant IDH1 R132H inhibitor, could be used in some biological studies.

CAS 1816331-63-1 GSK321

GSK321
(CAS: 1816331-63-1)

GSK321 is a highly potent, selective inhibitor of mutant IDH1 enzymes, with IC50= 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G. GSK321 st...

CAS 6147-11-1 alpha-Mangostin

alpha-Mangostin
(CAS: 6147-11-1)

Alpha-mangostin, a prenylated xanthone derivative from Mangosteen, Garcinia mangostana L. (Clusiaceae), has shown to possess diverse pharmacological activities ...

CAS 50405-58-8 TC-E 5008

TC-E 5008
(CAS: 50405-58-8)

TC-E 5008 is a selective and cancer-associated mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor (Ki = 120-190 nM), displaying >60-fold selectivity for mIDH1 ...

CAS 1429176-69-1 Mutant IDH1-IN-2

Mutant IDH1-IN-2
(CAS: 1429176-69-1)

Mutant IDH1-IN-2, aslo called as SCHEMBL14831158, is an inhibitor of mutant IDH protein. It is developed for the treatment of diseases associated with such muta...

Chemical Structure

CAS 1816331-63-1 GSK321

Quick Inquiry

Verification code

Featured Items