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1401033-86-0 (AMG 925)

1

Identification

AMG 925 AMG 925
Name AMG 925
Formula C26H29N7O2
MW 471.55
CAS No. 1401033-86-0
EINECS
Smiles OCC(N1CC2=C(N=C(NC3=NC=C4C(N([[email protected]]5CC[[email protected]](C)CC5)C6=CN=CC=C64)=N3)C=C2)CC1)=O
Synonyms AMG-925;AMG925; 2-hydroxy-1-(2-((9-((1r,4r)-4-methylcyclohexyl)-9H-pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidin-2-yl)amino)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)ethanone
InChI InChI=1S/C26H29N7O2/c1-16-2-5-18(6-3-16)33-22-13-27-10-8-19(22)20-12-28-26(31-25(20)33)30-23-7-4-17-14-32(24(35)15-34)11-9-21(17)29-23/h4,7-8,10,12-13,16,18,34H,2-3,5-6,9,11,14-15H2,1H3,(H,28,29,30,31)/t16-,18-
2

Introduction

AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell. IC50 value: 1.5/2.4 nM (CDK4/FLT3) Target: CDK4/FLT3 More information can be found in Patent WO 2012129344 A1 Fused tricyclic dual inhibitors of cdk 4/6 and flt3.

Background Information

Potent selective and orally available FLT3/CDK4 dual inhibitor ......by AOBIOUS INC
AMG-925 is a potent, selective, and bioavailable FLT3/cyclin-dependent kinase 4 (CDK4) dual kinase inhibitor. AMG 925 inhibited AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlated wit ......by BOC Sciences
AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with IC50s of 2±1 nM and 3±1 nM, respectively. ......by MedChemexpress Co., Ltd.
AMG-925 is a potent, selective, and bioavailable FLT3/cyclin-dependent kinase 4 (CDK4) dual kinase inhibitor. AMG 925 inhibited AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlated with the inhibition of STAT5 and RB phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, AMG 925 was also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and sorafenib). AMG 925, which combines inhibition of two kinases essential for proliferation and survival of FLT3-mutated AML cells, may improve and prolong clinical responses. (Mol Cancer Ther. 2014 Apr;13(4):880-9.)(05/16/2014) Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......by MedKoo Biosciences, Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000012006

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
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Mechanism and Indication

Signaling Pathways Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
Target CDK FLT3
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AMG 925 - Not Found
AMG 925 - No Development Reported
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Safety Data of AMG 925

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD36() USA
Active Biochem 5mg/USD130() USA
AdooQ BioScience, LLC 5mg/USD120() USA
Apexbio Technology LLC 5mg/USD105(In stock) USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD100();10mg/USD150() USA
DC Chemicals 100mg/USD450(In stock) China
MedChemexpress Co., Ltd. 5mg/USD100();10mg/USD150() USA
MedKoo Biosciences, Inc. 10mg/USD150() USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD100();10mg/USD150() China
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Related Products

Other Forms of 1401033-86-0

Name CAS No Formula MW

Recommended Compounds in CDK FLT3

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9
NU6102 444722-95-6 C18H22N6O3S 402.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

AMG 925

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