PI3K. 1

Transcription

1 PI3K PI3K (Phosphatidylinositol-4,5-bisphosphate 3-kinase) are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. Many of these functions relate to the ability of class I PI3-kinases to activate protein kinase B (PKB, Akt) as in the PI3K/AKT/mTOR pathway. The p110δ and p110γ isoforms regulate different aspects of immune responses. PI 3-kinases are also a key component of the insulin signaling pathway. PI3Ks are a family of related intracellularsignal transducer enzymes capable of phosphorylating the 3 position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns). 1

2 PI3K Inhibitors & Modulators 1,3-Dicaffeoylquinic acid (1,3-O-Dicaffeoylquinic aci d; 1,5-Dicaffeoylquinic acid) Cat. No.: HY-N Methyladenine (3-MA) Cat. No.: HY ,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative, and activates PI3K/Akt. 3-Methyladenine is a selective PI3K inhibitor with IC of 25 μm and 60 μm for Vps34 and PI3Kγ, respectively, and it can inhibit all PtdIns3Ks at 10 mm. Purity: 98.68% 5 mg, 10 mg, 25 mg Purity: 99.84% mg, 100 mg, 200 mg, 0 mg A66 (A 66; A-66) Cat. No.: HY Acalisib (GS-9820; GS9820; GS 9820; CAL-120; CAL120; CAL 120) Cat. No.: HY A66 is a highly specific and selective p110α inhibitor with IC of 32 nm. Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC value of 12.7 nm. Purity: 99.26% Purity: 99.94% Phase 1 AMG319 (AMG-319; AMG 319) Cat. No.: HY AS (AS ; AS252424) Cat. No.: HY AMG319 is a potent and selective PI3Kδ inhibitor with IC of 18 nm, also inhibits PI3Kγ with IC of 8 nm. AS is a potent and selective inhibitor of PI3Kγ with IC of 33 nm; >10 fold selectivity for PI3Kγ versus PI3Kα. Purity: 99.82% Phase 1, Phase 2 Purity: 98.29% 5 mg, 10 mg AS (AS605240; AS ) Cat. No.: HY AZD 6482 (AZD6482; AZD-6482; KIN-193; KIN 193; KIN193) Cat. No.: HY AS is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC = 8 nm) AZD6482 is a PI3Kβ inhibitor with IC of 10 nm, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ Purity: >98.00% 10 mg, mg, 100 mg AZD-8835 Cat. No.: HY AZD8186 (AZD-8186) Cat. No.: HY AZD8835 is a potent and selective inhibitor of PI3Kδ and PI3Kαwith IC of 5.7 nm and 6.2 nm, with selectivity against PI3Kβ (IC 431 nm) and PI3Kγ (IC 90 nm). AZD8186 is an isoform-specific small-molecule PI3K inhibitor, potently inhibits PI3Kβ (IC=4 nm) and PI3Kδ (IC=12 nm) with selectivity over PI3Kα (IC=35 nm) and PI3Kγ (IC=675 nm). Purity: 98.61% Phase 1 Purity: 99.92% Phase 1 2 Tel: Fax: sales@medchemexpress.com

3 BAY (BAY ; Copanlisib) Cat. No.: HY BEZ235 (NVP-BEZ 235; BEZ-235; BEZ 235; NVP-BEZ235) Cat. No.: HY-673 BAY is an ATP-competitive selective class-i PI3 kinases inhibitor, with IC s of 0.5, 0.7, 3.7 and 6.4 nm for PI3Kα, δ, β and γ, and much less active against mtor (IC =45 nm) and other PIKs (no inhibition at 1 μm). Phase 1, Phase 2 BEZ235 is a dual pan-class I PI3K and mtor kinase inhibitor with IC of 4 nm/5 nm/7 nm/75 nm, and 6 nm for p110α/ γ/ δ/ β and mtor ( p70s6k), respectively. Purity: 98.83% Phase 2 Size: mg, 100 mg, 200 mg, 0 mg BEZ235 (Tosylate) (NVP-BEZ 235 Tosylate; BEZ-235 Tosylate) Cat. No.: HY BYL-719 (Alpelisib; BYL 719; BYL719) Cat. No.: HY BEZ235 tosylate(nvp-bez235) is a dual ATP-competitive PI3K and mtor inhibitor for p110α/γ/δ/β and mtor(p70s6k) with IC of 4 nm/5 nm/7 nm/75 nm/6 nm, respectively; inhibits ATR with IC of 21 nm; shown to be poor inhibitory to Akt and PDK1 BYL-719 is a potent and selective PI3Kα inhibitor with IC of 5 nm. Phase 2 mg, 100 mg, 200 mg, 0 mg Purity: 99.04% Phase 2, 200 mg, 0 mg CAL-101 (CAL101; GS-1101; GS1101; GS 1101; CAL 101; Idelalisib) Cat. No.: HY CAL-130 (CAL130; CAL 130) Cat. No.: HY-16122A CAL-101 is a highly selective and potent p110δ inhibitor with IC of 2.5 nm, is 40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes ( p110α, p110β, and p110γ; IC are 820, 565, and 89nM, respectively). Purity: 98.38% Phase 3, 200 mg CAL-130 is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Size: CAL-130 (Hydrochloride) ((S)-2-(1-((2-amino-9H-purin-6-yl)amino )ethyl)-5-methyl-3-(o-tolyl)quinazolin-4(3h)-one ) Cat. No.: HY-16122B CAL-130 (Racemate) (CAL130 (Racemate); CAL 130 (Racemate)) Cat. No.: HY CAL-130 Hcl is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). CAL-130 racemate is a novel phosphoinositide 3-kinase (PI3K) inhibitor. It is reported that combined inhibition of PI3Kγ/δ as therapy for T cell acute lymphoblastic leukemia (T-ALL). Size: CAY105 (CAY 105; CAY-105) Cat. No.: HY CH (CH ; CH ) Cat. No.: HY CAY105 is a potent and selective PI3Kγ inhibitor with IC of 30 nm. CH selectively inhibits class I PI3Ks, such as PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC values of 0.014, 0.12, 0., and 0.36 um, respectively; shows less inhibition of class II PI3Ks, class III PI3ks, and mtor. 10 mg, 25 mg, mg, 100 mg Purity: 98.01% Phase 1 3

4 CNX-1351 Cat. No.: HY CUDC-907 (CUDC907; CUDC 907) Cat. No.: HY CNX-1351 is a potent and isoform-selective targeted covalent inhibitor of the lipid kinase PI3Kα with IC of 6.8 nm; times less potent against β, γ, and δ. CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with IC of 1.7/5.0/1.8/2.8 nm and 19/54/39 nm for HDAC1/2/3/10 and PI3Kα/β/δ, respectively. Purity: 99.44% Purity: 99.24% Phase 1 2 mg, CZC24832 (CZC 24832; CZC-24832) Cat. No.: HY Duvelisib (IPI-145; IPI 145; IPI145; INK1197; INK 1197; INK-1197) Cat. No.: HY CZC24832 is a selective inhibitor of PI 3-kinase γ (IC = 1.0 μm in a PI 3-Kγ-dependent fmlp-induced neutrophil migration assay); exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins. Duvelisib is a novel and selective PI3K δ/γ inhibitor with K i and IC of 23 pm/243 pm and 1 nm/ nm, highly selective for PI3K δ/γ than other protein kinases. Purity: 98.01% 5 mg, 10 mg Purity: 99.65% Phase 1, Phase 2 Duvelisib (R enantiomer) (IPI-145 R enantiomer; IPI 145 R enanti omer; IPI145 R enantiomer; INK1197 R enantiomer; ) Cat. No.: HY-17044A ETP (ETP 46321; ETP46321) Cat. No.: HY Duvelisib (R enantiomer) is a novel and selective PI3K δ/γ inhibitor with 2 ETP is a potent and orally bioavailable PI3K α/δ inhibitor with IC of 2.3/14.2 nm for p110α/p110β; exhibits potency on mutated p110α(ic= nm, p110a E542K; E545K; H1047R). Size: GDC-0032 (Taselisib; RG-7604; GDC0032; GDC 0032) Cat. No.: HY GDC-0084 (GDC0084; GDC 0084; RG7666; RG-7666; RG 7666) Cat. No.: HY GDC-0032 is a potent β-sparing small molecule inhibitor of PI3K, with IC values of 0.29 nm, 0.91 nm, 0.97 nm for PI3Kα, PI3Kβ and PI3Kγ, respectively. GDC-0084 is a potent, selective inhibitor of Class I PI3K and mtor with good penetration across the blood-brain barrier. Purity: 99.75% Phase 1, 200 mg Purity: 99.54% 1 mg, GDC-0941 (Pictilisib; GDC 0941; GDC0941) Cat. No.: HY-094 GDC-0941 (dimethanesulfonate) (Pictilisib dimethanesulfon ate; GDC-0941 (2 MeSO3H salt); GDC0941 dimethane ) Cat. No.: HY GDC-0941 is a potent inhibitor of PI3Kα/δ with IC of 3 nm, with modest selectivity against p110β (11-fold) and p110γ (25-fold). GDC MeSO3H salt is a potent inhibitor of PI3Kα/δ with IC of 3 nm, with modest selectivity against p110β (11-fold) and p110γ (25-fold) Purity: 99.52% Phase 1, Phase 2 10 mg, mg, 100 mg, 200 mg Purity: 99.57% Phase 1, Phase 2 10 mg, mg, 100 mg, 200 mg 4 Tel: Fax: sales@medchemexpress.com

5 GDC-0980 (GNE 390; GDC 0980; RG 7422) Cat. No.: HY GNE-317 Cat. No.: HY GDC-0980 is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC of 5 nm/27 nm/7 nm/14 nm in cell-free assays, respectively, and also a mtor inhibitor with K i of 17 nm in a cell-free assay, and highly selective versus other PIKK family kinases. Purity: 96.83% Phase 1, Phase 2 10 mg, mg, 100 mg GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood brain barrier; shows potent suppression of the PI3K pathway in the brain of mice with intact BBB. Purity: 98.46% GNE-477 (GNE477; GNE 477) Cat. No.: HY GNE-493 (GNE493; GNE 493) Cat. No.: HY GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC of 4 nm for PI3Kα, Kiapp is 21 nm for mtor. GNE-493 is a potent, selective, and orally available dual pan-pi3k/mtor inhibitor with ICs of 3.4/12/16/16/32 nm for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively. Purity: 98.45% 1 mg, 5 mg Purity: 98.19% 5 mg, 10 mg GSK (GSK ; GSK ) Cat. No.: HY GSK (Omipalisib; GSK-212; GSK ) Cat. No.: HY GSK is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mtor with IC of 0.4 nm/0.6 nm/2 nm/5 nm and 12 nm, respectively. GSK is a highly selective and potent inhibitor of PI3K with K i of nm/0.13 nm/0.024 nm/0.06 nm and 0.18 nm/0.3 nm for p110α/β/δ/γ, mtorc1/2, respectively. Purity: 98.07% 10 mg, mg, 100 mg Purity: 99.5% Phase 1 GSK (free base) (GSK free base; GSK free base) Cat. No.: HY-19535A GSK (GSK ; GSK ) Cat. No.: HY GSK (free base) is a potent and selective PI3Kδ inhibitor over the closely related isoforms. GSK is a potent, selective and orally bioavailable PI3Kβ inhibitor, sensitive to PTEN null cell lines. Purity: >98.0% 1 mg, 5 mg, 10 mg, 25 mg, mg, 100 mg Purity: 99.01% Phase 2 HS-173 (HS173; HS 173) Cat. No.: HY IC (IC87114; IC 87114) Cat. No.: HY HS-173 is a novel PI3K inhibitor, that is used for cancer treatment. IC was the first isoform-selective PI3K inhibitor. p110δ(ic = 0.13 μm) vs. p110α(ic = 200 μm), p110β(ic = 16 μm) and p110γ(ic = 61 μm). Purity: 99.32% 5 mg, 10 mg, 25 mg, mg Phase 3 5

6 INK-128 (Sapanisertib; MLN0128) Cat. No.: HY IPI549 (IPI-549; IPI 549) Cat. No.: HY INK-128 is a potent and selective mtor inhibitor with IC of 1 nm, > 200-fold less potent to class I PI3K isoforms, superior in blocking mtorc1/2 and sensitive to pro-invasion genes. IPI549 is a potent and selective PI3Kγ Inhibitor with IC of 16 nm. Purity: 99.55% Phase 1 Purity: >99.0% Phase 1 Isorhamnetin (3'-Methylquercetin) Cat. No.: HY-N0776 LY (NSC ; SF 1101; LY ; LY ) Cat. No.: HY Isorhamnetin is an O-methylated flavonol, a flavonoid aglucon. LY is a broad-spectrum inhibitor of PI3K, with IC of 0.5/0.57/0.97 μm for PI3Kα/δ/β, respectively, also potently inhibits CK2 with IC of 98 nm. Purity: 98% 5 mg, 10 mg, 25 mg, mg Purity: 99.97% Phase 1 10 mg, mg, 100 mg, 200 mg, 0 mg LY (LY ; LY ) Cat. No.: HY MLN1117 (INK1117; MLN-1117; INK-1117; MLN 1117; INK 1117) Cat. No.: HY LY is an oral ATP competitive inhibitor of the class I PI3K isoforms, mtor and DNA-PK, extracted from patent WO/ A1, compound example 1, has an IC of 64.9 nm, 42.1 nm, 10.6 nm, 19.1 nm for Akt1(pT308), Akt1 (ps473), P70S6(pT389), S6RP(pS240/242). Purity: 99.7% Phase 2 MLN1117 (INK1117) is a selective p110α inhibitor with IC of 15 nm. Purity: 99.87% Phase 1, Phase 2 5 mg, 10 mg, 25 mg, mg, 100 mg NVP-BAG956 (BAG 956) Cat. No.: HY NVP-BGT226 (NVP-BGT 226; NVP BGT 226) Cat. No.: HY NVP-BAG956(BAG 956) is a potent, ATP-competitive and selective dual PI3K and PDK1 inhibitor in vitro and in vivo,with IC values to be 56, 444, 34, 117 and 240 nm for PI3K p110 alpha, beta, delta and gamma and PDK1 kinases, respectively. NVP-BGT226(BGT 226) is a novel class I PI3K/mTOR inhibitor for PI3Kα/β/γ with IC of 4 nm/63 nm/38 nm Size: 10 mg, mg NVP-BKM120 (BKM-120; BKM120; BKM 120) Cat. No.: HY NVP-BKM120 (Hydrochloride) (BKM-120 hydrochloride; BKM 120 hydrochloride; BKM 120 hydrochloride) Cat. No.: HY NVP-BKM120 is a pan-class I PI3K inhibitor, with IC of 52 nm/166 nm/116 nm/262 nm for p110α/ β/ δ/ γ, respectively. NVP-BKM120 Hcl(BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC of 52 nm/166 nm/116 nm/262 nm, respectively. Reduced potency against VPS34, mtor, DNAPK, with little activity to PI4Kβ. Purity: 98.57% Phase 2, Phase 3, 200 mg, 0 mg Phase 2, Phase 3, Phase 4 6 Tel: Fax: sales@medchemexpress.com

7 NVP-QAV-572 (NVP-QAV 572) Cat. No.: HY ON (ON ; ON146040) Cat. No.: HY NVP-QAV-572 is a potent PI3K kianse inhibitor with IC of 10 nm. ON is the first dual PI3K and BCR-ABL inhibitor that targets the STAT3 and STAT5 pathways; inhibits PI3K α/δ isoforms with IC of 14/20 nm. Size: Size: PF (PF ; PF046912) Cat. No.: HY PF (PF ; PF ) Cat. No.: HY PF is a potent and selective inhibitor of PI3K and mtor kinases with antitumor activity. PF inhibits human and mouse PI3Kα with K i of 1.8 and 1.2 nm, respectively, human PI3K isoforms β, δ, and γ with K i of 2.1, 1.6, and 1.9 nm, respectively, and Purity: 98.58% human mtor wit Phase 1, Phase 2 PF is a potent and selective PI3K/mTOR dual kinase inhibitor with an IC() of 9.1nM. Purity: 98.88% 5 mg, 10 mg, 25 mg, mg PF Cat. No.: HY PI-103 (PI 103; PI103) Cat. No.: HY PF is a novel potent and selective PI3K inhibitor. PF inhibits PI3Kalpha (Ki=0.6 nm) and mtor (Ki=1440 nm). PI103 is a potent inhibitor with low IC values against recombinant PI3K isoforms p110alpha (IC= 2 nm), p110beta (IC= 3 nm), p110delta (IC= 3 nm), and p110gamma (IC= 15 nm), less potent to mtor/dna-pk with IC of 30 nm/23 nm Purity: 99.28% Phase 1, Phase 2 Size: PI-103 (Hydrochloride) (PI 103 hydrochloride; PI103 hydrochloride) Cat. No.: HY-10115A PI-3065 (PI3065; PI 3065) Cat. No.: HY PI103 is a potent inhibitor with low IC values against recombinant PI3K isoforms p110alpha (IC= 2 nm), p110beta (IC= 3 nm), p110delta (IC= 3 nm), and p110gamma (IC= 15 nm), less potent to mtor/dna-pk with IC of 30 nm/23 nm PI-3065 is a novel potent and selective PI3K p110δ inhibitor with IC of 15 nm; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mtor. Purity: 99.78% Phase 1, Phase 2 Purity: 98.27% PI3K inhibitor X PI3K-IN-1 Cat. No.: HY Cat. No.: HY PI3K inhibitor X is a derivative compound discovered by Exelixis Inc PI3K-IN-1 is a potent inhibitor of PI3K, more information can be found in patent WO A2 and WO A2 Purity: 98.06% 10 mg, mg 7

8 PI3Kα inhibitor 1 (5-Pyrimidinecarboxamide, N-hydroxy-2-[ methyl[[2-[6-(methylamino)-3-pyridinyl]-4-(4-mor ) Cat. No.: HY PI3Kγ inhibitor 1 Cat. No.: HY PI3Kα inhibitor 1 is a PI3Kα inhibitor extracted from patent US/ A1, compound 243, has an IC < 0.1 μm, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μm IC 1 μm). PI3Kγ inhibitor 1 is a potent PI3Kγ inhibitor. Purity: >98.0% Size: PI3kδ inhibitor 1 (2-[1-[[2-(5-Fluoro-1H-indol-4-yl)-4-(m orpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl ) Cat. No.: HY PIK-294 Cat. No.: HY PI3kδ inhibitor 1 is a potent and selective inhibitor of isoform of PI3Kδ; useful for treating disorders mediated by lipid kinases such as inflammation, immunol disorders, and cancer. PIK-294 is a highly selective p110δ inhibitor with IC of 10 nm, less potent to PI3Kα/β/γ. Size: 5 mg Purity: 99.79% PIK-90 (PIK90; PIK 90) Cat. No.: HY PIK-93 (PIK 93; PIK93) Cat. No.: HY PIK-90 is a PI3Kα/γ/δ inhibitor with IC of 11 nm/18 nm/58 nm, respectively, less potent to PI3Kβ(IC= 3 nm). PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC of 19 nm, and also inhibits PI3Kα with IC of 39 nm. Size: 10 mg, mg, 100 mg Purity: >98.00% PKI-402 (PKI 402; PKI402) Cat. No.: HY PKI-587 (Gedatolisib; PF ) Cat. No.: HY PKI-402 is a potent dual pan-pi3k/mtor inhibitor targeting PI3Kα/β/γ/δ and mtor with IC of 2 nm/7 nm/16 nm/14 nm and 3 nm, respectively; also potent to PI3Kα mutants E545K and H1047R. PKI-587(PF ) is a highly potent dual PI3K/mTOR kinase inhibitor with IC of 0 Purity: 99.16% Size: Phase 1, Phase 2 Size: PQR309 (PQR-309; PQR 309) Cat. No.: HY Quercetin Cat. No.: HY PQR309 is a PI3K inhibitor, inhibits ppkb and ps6 with "++++/+++(+)" in A2058 melanoma cell. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a inhibitor with of μm. PI3K IC Purity: 99.43% 2 mg, Purity: 98.21% 1 g, 5 g 8 Tel: Fax: sales@medchemexpress.com

9 SAR (Voxtalisib; XL765; SAR ; SAR ; XL 765; XL -765) Cat. No.: HY SAR405 (SAR-405; SAR 405) Cat. No.: HY SAR (XL765) is a potent and highly selective pan inhibitor of class I PI3Ks (α/β/γ/δ, IC=39/110/9/43 nm) with activity against mtor(ic= nm). SAR405 is highly potent and selective inhibitor of PIK3C3 with an IC of 27 nm. Purity: 98.43% Phase 1, Phase 2 5 mg, 10 mg, 25 mg, mg, 100 mg Purity: 98.1% 2 mg, 5 mg, 10 mg, 25 mg, mg TG (TG100115; TG ) Cat. No.: HY TGR-1202 (RP5264; TGR1202; TGR 1202; RP-5264; RP 5264) Cat. No.: HY TG is a PI3K γ and -δ inhibitor (IC = 83 and 235 nm, respectively) TGR-1202 is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC and EC values of 22.2 and 24.3 nm respectively. Purity: 99.12% Purity: >98.0% Phase 1 TGR-1202 (hydrochloride) (RP5264 hydrochloride; TGR1202 hydrochl oride; TGR 1202 hydrochloride; RP-5264 hydrochlo ) Cat. No.: HY-12279C TGR-1202 (R-enantiomer) (RP5264 R-enantiomer; TGR1202 R-enantiomer) Cat. No.: HY-12279F TGR-1202 hydrochloride is an orally available, next generation PI3Kdelta inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC and EC values of 22.2 and 24.3 nm respectively. TGR-1202 R-enantiomer is the R-enantiomer of TGR TGR-1202 is a PI3K inhibitor. Phase 1 Size: 2 mg, 5 mg TGX-221 (TGX221; TGX 221) Cat. No.: HY Vps34-IN-1 Cat. No.: HY TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β Vps34-IN-1 is a Vps34 inhibitor, extracted from patent WO/ A1, compound 16a, has an IC of 4 nm Purity: 99.78% 10 mg, mg, 100 mg Purity: 99.64% Vps34-PIK-III Cat. No.: HY VS-5584 (SB-2343; VS5584; VS 5584; SB2343; SB 2343) Cat. No.: HY Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC of 18 nm. VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mtor, PI3Kα/β/δ/γ with IC of 3.4 nm and nm, respectively. Size: Purity: 99.57% 9

10 Wortmannin (SL-2052; KY-12420) Cat. No.: HY XL-147 (SAR245408; XL 147; XL147; SAR ; SAR ; pil aralisib) Cat. No.: HY Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC s of 3 nm and 170 nm, respectively. XL147(SAR245408; pilaralisib) is a potent, orally bioavailable inhibitor of the class I PI3K family of lipid kinases with IC values of 39 nm/383 nm/36 nm/23 nm for PI3Kα/β/δ/γ, respectively; less potent to PI3Kβ. Purity: 99.33% 5 mg, 10 mg, 25 mg Purity: 98.35% Phase 2 ZSTK474 (ZSTK-474; ZSTK 474) Cat. No.: HY-847 ZSTK474 inhibits class I PI3K isoforms with IC of 37 nm, mostly PI3Kδ Purity: 99.56% Phase 1, Phase 2 10 mg, mg 10 Tel: Fax: sales@medchemexpress.com