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873436-91-0 (PU-H71)

1

Identification

PU-H71 PU-H71
Name PU-H71
Formula C18H21IN6O2S
MW 512.37
CAS No. 873436-91-0
EINECS
Smiles CC(C)NCCCN1C(SC2=C(C=C3OCOC3=C2)I)=NC4=C(N=CN=C14)N
Synonyms PU-H 71; PU H71; 8-((6-iodobenzo[d][1,3]dioxol-5-yl)thio)-9-(3-(isopropylamino)propyl)-9H-purin-6-amine
InChI InChI=1S/C18H21IN6O2S/c1-10(2)21-4-3-5-25-17-15(16(20)22-8-23-17)24-18(25)28-14-7-13-12(6-11(14)19)26-9-27-13/h6-8,10,21H,3-5,9H2,1-2H3,(H2,20,22,23)
2

Introduction

PU-H71 is a potent Hsp90 inhibitor with IC50 of 50 nM.

Background Information

PU-H71 is a potent potent inhibitor of heat shock protein 90. PU-H71 showed anti-tumor effects in TNBC xenografts, including complete response and tumor regression, without toxicity to the host are achieved with this agent. ......by BOC Sciences
PU-H71 is a potent Heat Shock Protein 90 (Hsp90) inhibitor (IC₅₀ = 50 nM). Also inhibits cell growth in a range of breast cancer cell lines (IC₅₀ values are 17, 31, 65, 87 and 140 nM for SKBr3, MCF-7, MDA-MB-468, HCC-1806 and MDA-MB-231 cells respectively). Shown to inhibit cell proliferation and induce apoptosis in triple-negative breast cancer (TNBC) cells. ......by BioVision, Inc.,
PU-H71 is discontinued. ......by MedKoo Biosciences, Inc.
A potent pan-HSP90 inhibitor with IC50s of 43/42/30/205 nM for Hsp90α/Hsp90β/Grp94/Trap-1 respectively; inhibits the growth of SKBr3 cell line and MDA-MB-468 cell line with IC50 of 50 nM and 58 nM respectively; significantly inhibits tumor growth in Ewing sarcoma xenografts.Bone CancerPhase 2 Clinical ......by ProbeChem
PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. ......by Selleck Chemicals LLC
Potent inhibitor of heat shock protein 90 (Hsp90) (IC50 = 51 nM in MDA-MB-468 cells). Also inhibits cell growth in a range of breast cancer cell lines (IC50 values are 17, 31, 65, 87 and 140 nM for SKBr3, MCF-7, MDA-MB-468, HCC-1806 and MDA-MB-231 cells respectively). Shown to inhibit cell proliferation and induce apoptosis in triple-negative breast cancer (TNBC) cells. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000028620

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.
Store at -20°C by Tocris Bioscience Inc.

Solubility

Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
Soluble to 100 mM in DMSO and to 100 mM in 1eq. HCl by Tocris Bioscience Inc.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
PU-H71 National Cancer Institute Non-Hodgkin lymphoma 2011/4/30 2013/4/30 Phase 1 Clinical
PU-H71 National Cancer Institute Solid tumor 2011/4/30 2013/4/30 Phase 1 Clinical
PU-H71 Memorial Sloan-Kettering Cancer Center Cancer 2011/7/31 2014/7/31 Phase 1 Clinical
PU-H71 - No Development Reported
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Safety Data of PU-H71

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Spectral Information

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Suppliers List

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Related Products

Other Forms of 873436-91-0

Name CAS No Formula MW
PU-H71 Hydrate(1:x) 1202865-65-3 C18H21IN6O2S 512.37

Recommended Compounds in HSP

Name CAS No Formula MW
VER-49009 558640-51-0 C19H18ClN3O4 387.82
VER-50589 747413-08-7 C19H17ClN2O5 388.8
Debio 0932 1061318-81-7 C22H30N6O2S 442.58
17-AAG (Hydrochloride) 911710-03-7 C31H44ClN3O8 622.15
Ganetespib 888216-25-9 C20H20N4O3 364.4
NVP-HSP990 934343-74-5 C20H18FN5O2 379.39
PF-4942847 1207961-29-2 C20H17Cl2F4N7O2 534.29
Apoptozole 1054543-47-3 C33H25F6N3O3 625.5603
AT13387 912999-49-6 C24H31N3O3 409.52
XL888 1149705-71-4 C29H37N5O3 503.64
1134156-31-2
Alvespimycin 467214-20-6 C32H48N4O8 616.75
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Geldanamycin 30562-34-6 C29H40N2O9 560.64
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Triptolide 38748-32-2 C20H24O6 360.4
PF-04929113 908115-27-5 C25H30F3N5O4 521.53
NVP-BEP800 847559-80-2 C21H23Cl2N5O2S 480.41
BIIB021 848695-25-0 C14H15ClN6O 318.76

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
CAL-101 870281-82-6 C22H18FN7O 415.42
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Nordihydroguaiaretic acid 500-38-9 C18H22O4 302.36
Pazopanib (Hydrochloride) 635702-64-6 C21H24ClN7O2S 473.98
RX-3117 865838-26-2 C10H12FN3O4 257.22
N-Hydroxy-3-(3-phenylsulfamoylphenyl)acrylamide 414864-00-9 C15H14N2O4S 318.34766
OSU-03012 742112-33-0 C26H19F3N4O 460.45
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Octreotide (acetate) 79517-01-4 C51H70N10O12S2 1079.29
LY2603618 911222-45-2 C18H22BrN5O3 436.3
AT13387 912999-49-6 C24H31N3O3 409.52
Dasatinib (hydrochloride) 854001-07-3 C22H27Cl2N7O2S 524.47
Delanzomib 847499-27-8 C21H28BN3O5 413.28
SU14813 (maleate) 849643-15-8 C27H31FN4O8 558.56
LY2090314 603288-22-8 C28H25FN6O3 512.53
XL-647 781613-23-8 C24H25Cl2FN4O2 491.39
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Route of Synthesis

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References

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More Information

PU-H71

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