CAS NO. |
Products Name |
201943-63-7 |
LY341495 |
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LY341495 is a highly potent and selective group II metabotropic glutamate receptor antagonist. (Ki/IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu2, mGlu3, mGlu8 , mGlu7a, mGlu1a, mGlu5a and mGlu4a receptors respectively). |
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1071992-99-8 |
AT406 (SM-406, ARRY-334543) |
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AT-406 (formerly known as SM-406) is an orally bioavailable potent IAP (inhibitor of apoptosis protein) of XIAP, cIAP1, and cIAP2 with Ki of 66.4 nM, 1.9 nM, and 5.1 nM, respectively. |
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1021868-92-7 |
ZM39923 HCL |
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ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. |
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934162-61-5 |
A-966492 |
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A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
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1225278-16-9 |
DCC-2618 |
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Description: IC50 Value: 6 nM and 9 nM for wt c-KIT and KIT V654A exon 13 respectively; 30 nM and 13 nM for PDGFR alpha and beta respectively [1]. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamembrane domain mutants (JMD) as well as secondary resistant KIT kinase-domain mutants. DCC-2618 additionally targets PDGFR alpha oncogenic mutants [1]. Deciphera's technology has identified DCC-2618 as a molecule which can be developed as second line therapy for imatinib and sunitinib resistant GIST patients with the potential to progress to frontline GIST therapy. in vitro: DCC-2618 inhibits normal and mutant KIT kinase at the nanomol level. The targets are wt c-KIT, c-KIT mutants, PDGFR alpha, PDGFR beta, KDR and cFMS. DCC-2618 inhibits mutant KIT in GIST patient cell line (GIST T1 pKIT western Ex11 deletion) at a IC 50 of 2 nM [1]. |
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1001645-58-4 |
SRT1720 |
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SRT1720 is a selective SIRT1 activator with EC50 of 0.16 μM, but is >230-fold less potent for SIRT2 and SIRT3. |
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905586-69-8 |
AZ960 |
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AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. |
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943540-75-8 |
JNJ-38877605 |
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JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. |
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1214265-57-2 |
WZ8040 |
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WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). |
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