ChemicalBook >> CAS DataBase List >>1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

CAS No.
1092788-83-4
Chemical Name:
1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Synonyms
CS-431;PP 121;PP121;PP-121;PP121 >=98% (HPLC);PTK/PI 3-K/mTOR Inhibitor, PP121;PP-121 PTK PI 3-K mTOR Inhibitor PP121;4-(Pyridin-3-yl) pyriMidin-2-aMine IMatinib;PTK/PI 3-K/mTOR Inhibitor, PP121 - CAS 1092788-83-4 - Calbiochem;1-cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)pyrazolo[3,4-d]pyrimidin-4-amine;1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
CBNumber:
CB42509990
Molecular Formula:
C17H17N7
Molecular Weight:
319.36
MDL Number:
MFCD12912434
MOL File:
1092788-83-4.mol
Last updated:2023-09-20 16:43:00

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Properties

Density 1.63
storage temp. 2-8°C
solubility DMSO: >10mg/mL
form White solid
pka 12.79±0.40(Predicted)
color off-white
FDA UNII 5B9VB06146

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P280-P305+P351+P338
Hazard Codes  Xn
Risk Statements  22
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  1
NFPA 704
0
2 0

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine price More Price(32)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich P0036 PP121 ≥98% (HPLC) 1092788-83-4 5mg $211 2024-03-01 Buy
Sigma-Aldrich 529584 PTK/PI 3-K/mTOR Inhibitor, PP121 1092788-83-4 5mg $187 2024-03-01 Buy
Cayman Chemical 21196 PP121 ≥98% 1092788-83-4 5mg $81 2024-03-01 Buy
Cayman Chemical 21196 PP121 ≥98% 1092788-83-4 10mg $130 2024-03-01 Buy
Sigma-Aldrich P0036 PP121 ≥98% (HPLC) 1092788-83-4 25mg $746 2022-05-15 Buy
Product number Packaging Price Buy
P0036 5mg $211 Buy
529584 5mg $187 Buy
21196 5mg $81 Buy
21196 10mg $130 Buy
P0036 25mg $746 Buy

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Chemical Properties,Uses,Production

Uses

PP-121 is a multi-target inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, respectively, and also inhibits DNA-PK with IC50 of 60 nM.

Definition

ChEBI: PP121 is a pyrazolopyrimidine that is 1H-pyrazolo[3,4-d]pyrimidine which is substituted by a cyclopentyl, 1H-pyrrolo[2,3-b]pyridin-5-yl, and amino groups at positions 1, 3 and 4, respectively. It is a dual inhibitor of tyrosine and phosphoinositide kinases and exhibits anti-cancer properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a tyrosine kinase inhibitor and an antineoplastic agent. It is a pyrazolopyrimidine, a pyrrolopyridine, a member of cyclopentanes and an aromatic amine.

General Description

A cell-permeable pyrazolopyrimidine compound that effectively targets the ATP pocket of both protein tyrosine kinases (IC50<0.26 M against Abl, EGFR, EphB4, Hck, PDGFR, RET, Src, SrcT338I, and VEGFR2) and PI 3-K family kinases (IC50<1.4 M against p110α/ β/ δ/ γ, mTOR, and DNA-PK). PP121 is less effective against ser/thr kinases and exhibits significant inhibition of only 14 ser/thr kinases (≥70% inhibition with 1 M inhibitor and 10 M ATP) in a 219 kinase panel screening. Individually targeting Ret by sorafenib (IC50 = 780 nM) or PI 3-K/mTOR pathway by PI-103 (IC50 = 800 nM) is shown to be less effective than PP121 treatment (IC50 = 50 nM) in inhibiting the proliferation of Ret C634W-expressing TT thyroid carcinoma cultures.

Biological Activity

pp121 is a dual inhibitor of tyrosine and phosphoinositide kinases [1].pp121 is found to inhibit both tyrosine kinases and pi3-ks but not serine-threonine kinases. it potently inhibits p110α, p110β, p110γ, p110δ, dna-pk and mtor with ic50 values of 52nm, 1.4μm, 1.1μm, 150nm, 60nm and 10nm, respectively. for the tyrosine kinases, pp121 shows inhibition with ic50 values of 21nm, 4nm, 10nm,55nm, 550nm, 220nm and <1nm for ab1, hck, src, vegfr2, egfr, ephb4 and pdgfr, respectively [1].in cells, pp121 can reverse v-src mediated cellular transformation and restore actin stress fiber staining. pp121 also potently inhibits the mutant ret kinase with ic50 value less than 1nm in thyroid tumors34. furthermore, pp121 is found to evade drug resistance through redundantly targeting bcr-abl mediated cell survival and pi3-k/mtor mediated cell proliferation [1].

Biochem/physiol Actions

PP121 is a dual inhibitor of tyrosine and phosphoinositide kinases. PP121 is the first inhibitor active on both Tyrosine kinases and the phosphatidylinositol-3-OH kinase (PI(3)K) family. The inhibitor is not effecting other serine-threonine protein kinases.

storage

Store at -20°C

References

[1] apsel b, blair j a, gonzalez b, et al. targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. nature chemical biology, 2008, 4(11): 691-699.

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 113)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co
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Hubei Jusheng Technology Co.,Ltd.
18871490254 linda@hubeijusheng.com CHINA 28180 58
Chongqing Chemdad Co., Ltd
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CONIER CHEM AND PHARMA LIMITED
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TargetMol Chemicals Inc.
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
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Dideu Industries Group Limited
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Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58

View Lastest Price from 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine pictures 2019-07-06 1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
1092788-83-4
US $2.00 / kg 1kg 99% 100kg Career Henan Chemical Co

1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Spectrum

1092788-83-4(1-Cyclopentyl-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine)Related Search:

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