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1204144-28-4 (AZD1208)

1

Identification

AZD1208 AZD1208
Name AZD1208
Formula C21H21N3O2S
MW 379.48
CAS No. 1204144-28-4
EINECS
Smiles O=C(NC/1=O)SC1=C/C2=C(N3C[[email protected]](N)CCC3)C(C4=CC=CC=C4)=CC=C2
Synonyms AZD 1208;AZD-1208; (R,Z)-5-((2-(3-aminopiperidin-1-yl)-[1,1'-biphenyl]-3-yl)methylene)thiazolidine-2,4-dione
InChI InChI=1S/C21H21N3O2S/c22-16-9-5-11-24(13-16)19-15(12-18-20(25)23-21(26)27-18)8-4-10-17(19)14-6-2-1-3-7-14/h1-4,6-8,10,12,16H,5,9,11,13,22H2,(H,23,25,26)/b18-12-/t16-/m1/s1
2

Introduction

AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML. IC50 Value: < 5 nM Target: pan-Pim kinase AZD1208 suppresses the growth of MOLM 16 and KG 1 xenograft tumors in vivo in a dosedependent manner.

Background Information

A novel, orally bioavailable, highly selective PIM kinases inhibitor with single nanomolar potency against all three PIM kinases ......by AOBIOUS INC
AZD-1208 is a potent and selective pan-Pim kinase inhibitor which demonstrates efficacy in preclinical models of acute myeloid leukemia. AZD1208 inhibited the growth of 5 of 14 acute myeloid leukemia (AML) cell lines tested, and sensitivity correlates with Pim-1 expression and STAT5 activation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells, accompanied by a dose-dependent reduction in phosphorylation of Bcl-2 antagonist of cell death, 4EBP1, p70S6K, and S6, as well as increases in cleaved caspase 3 and p27.AZD1208 inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo with a clear pharmacodynamic-pharmacokinetic relationship. AZD1208 also potently inhibits colony growth and Pim signaling substrates in primary AML cells from bone marrow that are Flt3 wild-type or Flt3 internal tandem duplication mutant.AZD1208 inhibited tumorigenesis in tissue recombinants, Myc-CaP, and human PC xenograft models.AZD1208 suppressed multiple protumorigenic pathways, including the MYC gene program. ......by AbMole BioScience
AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. AZD1208 inhibits the activities of PIM1, PIM2 and PIM3 serine/threonine kinases, which may result in the interruption of the G1/S phase cell cycle ......by BOC Sciences
AZD1208 is a potent and highly selective pan-Pim Kinase inhibitor. It inhibits Pim-1,-2, and -3 kinases at <5 nM or <150 nM in enzyme and cell assays, respectively. Displays potent anticancer activities. ......by BioVision, Inc.,
AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor. ......by MedChemexpress Co., Ltd.
AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity. Pan-PIM kinase inhibitor AZD1208 inhibits the activities of PIM1, PIM2 and PIM3 serine/threonine kinases, which may result in the interruption of the G1/S phase cell cycle transition, thereby causing cell cycle arrest and inducing apoptosis in cells that overexpress PIMs. The growth inhibition of several leukemia cell lines by this agent is correlated with the expression levels of PIM1, which is the substrate of STAT transcription factors. PIM kinases are downstream effectors of many cytokine and growth factor signaling pathways and are upregulated in various malignancies. ......by MedKoo Biosciences, Inc.
AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. Phase 1. ......by Selleck Chemicals LLC
AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML. AZD1208 suppresses the growth of MOLM 16 and KG 1 xenograft tumors in vivo in a dosedependent manner. Furthermore, AZD1208 leads to potent inhibition of colony development of primary AML cells from bone marrow aspirates and downregulates the phosphorylation of PIM goals. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of PIM1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. ......by Target Molecule Corp.
Potent pan Pim kinase inhibitor (IC50 values are 0.4, 1.9 and 5.0 nM for Pim-1, 3 and 2, respectively). Exhibits >43-fold higher affinity for Pim kinases over a range of other kinases. Induces cell cycle arrest and apoptosis in AML cell lines in vitro and inhibits growth of tumor xenografts in vivo. Chemosensitizer. ......by Tocris Bioscience Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000015422

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

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AZD1208 AstraZeneca plc Lymphoma 2012/7/31 2013/12/31 Phase 1 Clinical
AZD1208 AstraZeneca plc Advanced solid tumor 2012/7/31 2013/12/31 Phase 1 Clinical
AZD1208 AstraZeneca plc Acute myelogenous leukemia 2012/2/29 2015/1/31 Phase 1 Clinical
AZD1208 AstraZeneca plc Advanced solid tumor 2012/7/31 2013/12/31 Phase 1 Clinical
AZD1208 AstraZeneca plc Acute myelogenous leukemia 2012/2/29 2015/1/31 Phase 1 Clinical
AZD1208 - Phase 1
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Safety Data of AZD1208

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC 10mg/USD133(In stock) USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., 1mg/USD85() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD72();10mg/USD102() USA
Cayman Chemical Company USA
MedChemexpress Co., Ltd. 5mg/USD72();10mg/USD102() USA
MedKoo Biosciences, Inc. 1mg/USD50() USA
Selleck Chemicals LLC 10mg/USD134(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD72();10mg/USD102() China
Target Molecule Corp. 10mg/USD96();50mg/USD280() USA
Tocris Bioscience Inc. USA
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Related Products

Other Forms of 1204144-28-4

Name CAS No Formula MW

Recommended Compounds in Pim

Name CAS No Formula MW
CX-6258 (hydrochloride hydrate) 1353858-99-7 C26H27Cl2N3O4 516.42
CX-6258 1202916-90-2 C26H24ClN3O3 461.94
TCS PIM-1 1 491871-58-0 C18H11BrN2O2 367.2
TCS-PIM-1-4a 327033-36-3 C11H6F3NO2S 273.23
(Z)-SMI-4a 438190-29-5 C11H6F3NO2S 273.231
SGI-1776 1025065-69-3 C20H22F3N5O 405.42
Pim1/AKK1-IN-1 1093222-27-5 C20H13N5O 339.3501
Hispidulin 1447-88-7 C16H12O6 300.26
PIM447 1210608-43-7 C24H23F3N4O 440.4608
GDC-0339 1428569-85-0 C20H22F3N7OS 465.5
PIM-447 (hydrochloride) 1210416-52-6 C24H24ClF3N4OX 476.92
M-110 1395048-49-3 C22H28ClN5O3 445.94
PIM-447 (dihydrochloride) 1820565-69-2 C24H25Cl2F3N4O 513.38
TP-3654 1361951-15-6 C22H25F3N4O 0.0
SMI-16a 587852-28-6 C13H13NO3S 263.31
PIM inhibitor 1 (phosphate) 2088852-47-3 C26H29F3N5O7P 611.51
(1S,3R,5R)-PIM447 (dihydrochloride) C24H25Cl2F3N4O 513.3827096
AZD1208 hydrochloride 1621866-96-3 C21H22ClN3O2S 415.93628
NJC97-NH C22H14N2O3 354.36
HS56 C14H9ClN4OS 316.77

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
AZD1152-HQPA 722544-51-6 C26H30FN7O3 507.56
Mocetinostat 726169-73-9 C23H20N6O 396.44
OSI-930 728033-96-3 C22H16F3N3O2S 443.44
Volasertib 755038-65-4 C34H50N8O3 618.81
AT7867 857531-00-1 C20H20ClN3 337.85
NVP-BGJ398 872511-34-7 C26H31Cl2N7O3 560.48
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
Bleomycin (sulfate) 9041-93-4 C110H168N34O46S7 2927.17
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
ABC294640 915385-81-8 C23H25ClN2O 380.91
OTSSP167 1431697-89-0 C25H28Cl2N4O2 487.42
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
ZSTK474 475110-96-4 C19H21F2N7O2 417.41
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Route of Synthesis

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References

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More Information

AZD1208

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